g-quadruplex ligand telomestatin: Topics by WorldWideScience.org

Ligands in PSI structures

Molecular dynamics simulations have been used to study the differences between two DNA and RNA 14-mer quadruplexes of analogous sequences. Their structures present a completely different fold: DNA forms a bimolecular quadruplex containing antiparallel strands and diagonal loops; RNA forms an intrastrand parallel quadruplex containing a G-tetrad and an hexad, which dimerizes by hexad stacking. We used a multiscale computational approach combining classical Molecular dynamics simulations and density functional theory calculations to elucidate the difference in stability of the 2-folds and their ability in coordinating cations. The presence of 2'-OH groups in the RNA promotes the formation of a large number of intramolecular hydrogen bonds that account for the difference in fold and stability of the two 14-mers. We observe that the adenines in the RNA quadruplex play a key role in conserving the geometry of the hexad. We predict the cation coordination mode of the two quadruplexes, not ...

2008-09-03

One-step RNA pathogen detection with reverse transcriptase activity of a mutated thermostable Thermus aquaticus DNA polymerase.

Approximately 65% of PSI structures report some type of ligand(s) that is bound in the crystal structure. Here, a description is given of how such ligands are handled and analyzed at the JCSG and a...Full Text Available

Lineage-specific co-evolution of the Egf receptor/ligand signaling system

We describe the cloning and characterization of a mutated thermostable DNA polymerase from Thermus aquaticus (Taq) that exhibits an increased reverse transcriptase activity and is therefore designated for one-step PCR pathogen detection using established real-time detection methods. We demonstrate that this Taq polymerase mutant (Taq M1) has similar PCR sensitivity and nuclease activity as the respective Taq wild-type DNA polymerase. In addition, and in marked contrast to the wild-type, Taq M1 exhibits a significantly increased reverse transcriptase activity especially at high temperatures (>60 degrees C). RNA generally hosts highly stable secondary structure motifs, such as hairpins and G-quadruplexes, which complicate, or in the worst case obviate, reverse transcription (RT). Thus, RT at high temperatures is desired to weaken or melt secondary structure motifs. To demonstrate the ability of Taq M1 for RNA detection of pathogens, we performed TaqMan probe-based ...

2010-02-01

Technetium complexes based on tridentate/monodentate ligands - a new approach to brain imaging agents?

BackgroundThe epidermal growth factor receptor (Egfr) with its numerous ligands has fundamental roles in development, cell differentiation and physiology. Dysfunction of the receptor-ligand...Full Text Available

Multinuclear Magnetic Resonance and X-ray Crystallographic Investigation of Some Mixed Ligand Alkylisocynaide Platinum(Ii) Complexes

Abstract only.

Inertial Dynamic Effect on the Rates of Diffusion-Controlled Ligand-Receptor Reactions

No abstract prepared.

2005-08-01

KoreaScience (Korea)

Full Text Available

2011-08-01

In situ ligand exchange of thiol-capped CuInS2/ZnS quantum dots at growth stage without affecting luminescent characteristics

British Library Electronic Table of Contents (United Kingdom)

An aliphatic thiol ligand of CuInS2/ZnS core/shell quantum dots is replaced with a hydroxyl-terminated thiol ligand by utilizing `on-off state' of ligands during growth stage of the quantum dots. After the ligand-exchange, negligible differences were observed on both photoluminescence spectrum and luminescent quantum efficiency. The reason for the high retention of luminescent efficiency comes from no local agglomeration and no surface deterioration of QDs. It is also observed that 70% of initial ligands are exchanged by the replacing ligand, determined by FT-IR and 1H NMR. The proposed method provides the quantum dots with an excellent dispersibility in polar solvents, supported by identical luminescence decay characteristics of the QDs.

2011-01-01

Prolonged signaling at the parathyroid hormone receptor by peptide ligands targeted to a specific receptor conformation

No Effect of the Altered Peptide Ligand NBI-6024 on ?-Cell Residual Function and Insulin Needs in New-Onset Type 1 Diabetes

The parathyroid hormone receptor (PTHR) is a class B G protein-coupled receptor that plays critical roles in bone and mineral ion metabolism. Ligand binding to the PTHR involves interactions to both...Full Text Available

2008-10-28

Induction of Oxidative Stress Responses by Dioxin and other Ligands of the Aryl Hydrocarbon Receptor

OBJECTIVEThis randomized, four-arm, placebo-controlled, dose-ranging phase 2 trial was conducted to determine whether repeated subcutaneous injections of the altered peptide ligand,...Full Text Available

2009-11-01

Dynamics of ligand substitution in labile cobalt complexes resolved by ultrafast T-jump

TCDD and other polyhalogenated aromatic hydrocarbon ligands of the aryl hydrocarbon receptor (AHR) have been classically considered as non-genotoxic compounds because they fail to be directly mutagenic...Full Text Available

Universal spectrochemical series of six-coordinate octahedral metal complexes for modifying the ligand field splitting.

Ligand exchange of hydrated metal complexes is common in chemical and biological systems. Using the ultrafast T-jump, we examined this process, specifically the transformation of aqua cobalt (II) complexes...Full Text Available

2008-09-02

The effect of phosphonic acid substituents on europium(III) complex stability in acidic solutions

We studied a novel universal spectrochemical series of six-coordinated octahedral 3d transition metal complexes, which can be used for any combination of central metal atom and ligand molecules. A two dimensional spectrochemical series could be used to estimate the ligand field splitting energy of not only known compounds but also the unknown compounds. Therefore, it should be possible to control the physical properties, such as the electronic and magnetic properties and the optical phenomena of octahedral transition metal complexes by modifying the ligand field splitting. PMID:19378561

2009-01-28

Synthesis, Chemical Characterization and Catalytic Activity of Transition Metal Complexes Having Imine Based Nitrogen Donor Ligand

The thermodynamics of protonation and europium(III) complex formation with substituted methane diphosphonic acids have been reported recently. These ligands form strong complexes with europium in moderately acidic solutions ((H{sup +}) {ge} 0.1 M), conditions not conducive to complexation by most carboxylate and aminopolycarboxylate ligands. A correlation of log {beta} vs pK{sub a} values for phosphonate and carboxylate ligands is used to explore the effect of ligand structure on complex stability. 5 refs., 1 fig.

1990-01-01

KoreaScience (Korea)

Full Text Available

2010-02-01

Preparation and evaluation of Tc-99m complexes of aromatic bridged amine-amide-thiol-thioether N_2S_2 ligands

Platinum Acetylide Two-Photon Chromophores (Preprint)

Short communication.

Molecular recognition of nitrated fatty acids by PPAR[gamma

... ligands. Wavelength maxima and molar extinction coefficients are given in Tables 1 and 2. Compared to their 9 Page 14. ...

2007-04-01

Spin transition in octahedral metal complexes containing tetraazamacrocyclic ligands

Peroxisome proliferator activated receptor-{gamma} (PPAR{gamma}) regulates metabolic homeostasis and adipocyte differentiation, and it is activated by oxidized and nitrated fatty acids. Here we report the crystal structure of the PPAR{gamma} ligand binding domain bound to nitrated linoleic acid, a potent endogenous ligand of PPAR{gamma}. Structural and functional studies of receptor-ligand interactions reveal the molecular basis of PPAR{gamma} discrimination of various naturally occurring fatty acid derivatives.

2010-03-08

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16

British Library Electronic Table of Contents (United Kingdom)

This review focusses on spin crossover complexes with octahedral metal ions which are bound to a tetraazamacrocyclic ligand and additionally either to two monodentate ligands or to one bidentate ligand. Macrocyclic ligands with a sufficiently large ring size prefer to coordinate to metal ions in an equatorial fashion yielding trans-octahedral coordination environments. In contrast, twelve-membered tetraazamacrocycles with high steric rigidity, such as 2,11-diaza[3.3](2,6)pyridinophanes or 2,11-dithia[3.3](2,6)pyridinophane, are prone to form cis-octahedral complexes. While the electronic and the steric properties of the coordinated tetraazamacrocycle in trans-octahedral complexes are very likely responsible for the paucity of observed spin transitions, the cis-octahedral coordination mode ...

2009-01-01

Mixed-ligand complexes of scandium with 4-(2-pyridylazo)resorcinol and monocarboxylic acids

Kinetic manifestation of cooperative interaction between quinuclidinyl benzilate and rat brain muscarine cholinoreceptors

Scandium reacts with 4-(2-pyridylazo)resorcinol in the presence of monocarboxylic acids (X) to form mixed-ligand complexes with a Sc:PAR:x ratio of 1:2:2. The chemical nature of this interaction has been established, and the extraction of these mixed-ligand complexes has also been investigated; stability constants and molar extinction coefficients have been calculated. The values of the latter decrease in the order CH_3COOH > CH_2ClCOOH > CCl_3COOH. The formation and extraction of mixed-ligand complexes in Sc-PAR-HX systems make it possible to increase the sensitivity and selectivity of scandium determination in comparison with the use of the Sc-PAR mono-ligand complex.

1987-09-01

Architectural design criteria for f-block metal ion sequestering agents. 1998 annual progress report

A study was made of the kinetics of L-(/sup 3/H)quinuclidinyl benzilate binding with membrane-bound muscarine cholinoreceptors from the rat brain. Determination was made of the rate constants of this process, and constants as a function of ligand concentration was investigated, indicating that there is a complex mechanism of interaction of antagonists with muscarine receptor. With up to 3.5 nM concentrations of L-(/sup 3/H)quinuclidinyl benzilate, the binding reaction occurs in two stages: rapid equilibrated binding is followed by a slow process of conformational isomerization of the receptor-ligand complex. At higher ligand concentrations, there is additional drastic increase in constant of rate of ligand binding a new plateau is reached. Such dependence of rate constant on ligand concentration is indicative of the cooperative nature of interaction between antagonists and muscarine ...

1985-01-01

Metal coordination and selectivity with oxine ligands bound to silica polyamine composites

'The objective of this project is to provide a means to optimize ligand architecture for f-block metal recognition. The authors strategy builds on an innovative and successful molecular modeling approach in developing polyether ligand design criteria for the alkali and alkaline earth cations. The hypothesis underlying this proposal is that differences in metal ion binding with multidentate ligands bearing the same number and type of donor groups are primarily attributable to intramolecular steric factors. They propose quantifying these steric factors through the application of molecular mechanics models. The research involves close integration of theoretical and experimental chemistry. The experimental work entails synthesizing novel ligands and experimentally determining structures and binding constants for metal ion complexation by series of ligands in which architecture ...

1998-12-31

British Library Electronic Table of Contents (United Kingdom)

A series of oxine ligands, 5-X, 8 OH C9H6N (X = H, Cl, SO3H) have been covalently bound to a silica gel polyamine composite made from a silanized amorphous silica xerogel and poly(allylamine) (BP-1) by the Mannich reaction. The resulting modified composites WP-4(X = H), CB-1(X = Cl), and SB-1(X = SO3H) were characterized by elemental analysis, FTIR, and solid state CPMAS-13C-NMR. Using the analytical data before and after the ligand modification, the ligand loading could be estimated and in combination with metal ion capacities a metal to ligand ratio could be obtained. The composites WP-4 and CB-1 both showed ratios of approximately 1 : 1 while the sulfonate modified composite, SB-1, showed a metal to ligand ratio of 1 : 2. This is tentatively interpreted in terms of a zwitterionic oxine ...

2010-01-01

Mixed-ligand tungsten-antipyrine-trihydroxyfluorone complexes and their use in analysis

First investigations of complex formation of At(I) with phosphorous organic compounds

In order to increase the sensitivity of photometric determination of tungsten and to find forms with high molar extinction coefficients, mixed-ligand complexes of tungsten with antipyrine and trihydroxyfluorone have been studied. The molar extinction coefficients have been determined for chloride associates of mixed-ligand complexes containing different trioxyfluorones: phenylfluorone, salicylflourone, p-bromphenylfluorone, anthrafluorone, dioxyfluorescein, and dioxyfluoroscein ethylate (DOFE). An associate formed by DOFE has the maximum molar extinction coefficient. It has been used for photometric determination of microgram amounts of tungsten impurity in vanadyl sulphate.

1977-01-01

First investigations of complex formation of At(I) with phosphorous organic compounds

Reaction of At(I) with triphenylphosphine, triethylphosphite and tri-n-octylphosphine oxide was investigated in ethanolic solution by means of electromigration. A cationic complex with triphenylphosphine was identified being stable at pH = 1,9 in the concentration range of the ligand between c = 10{sup -5} to 10{sup -3} M. At a higher ligand concentration and at pH>2, the reduction effect of phosphine is superimposed on the complex formation. Complex formation is confirmed by ligand exchange reactions with Br{sup -} and I{sup -}. A comparatively weak complex is formed by triethylphosphite and At(I). No compound is formed by tri-n-octylphosphine oxide and At(I). (orig.).

1989-01-01

Synthesis and characterization of platinum(II) complexes containing tetracycline derivatives like ligands; Sintese e caracterizacao de complexos de platina(II) contendo derivados de tetraciclina como ligantes

Reaction of At(I) with triphenylphosphine, triethylphosphite and tri-n-octylphosphine oxide was investigated in ethanolic solution by means of electromigration. A cationic complex with triphenylphosphine was identified being stable at pH = 1,9 in the concentration range of the ligand between c = 10"-"5 to 10"-"3 M. At a higher ligand concentration and at pH>2, the reduction effect of phosphine is superimposed on the complex formation. Complex formation is confirmed by ligand exchange reactions with Br"- and I"-. A comparatively weak complex is formed by triethylphosphite and At(I). No compound is formed by tri-n-octylphosphine oxide and At(I). (orig.).

Small and neutral Tc"vO BAT, bisaminoethanethiol (N_2S_2) complexes for developing new brain imaging agents

No abstract prepared.

2005-07-01

SAR of Cu (II) Thiosemicarbazone Complexes as Hypoxic Imaging Agents: MM3 Analysis and Prediction of Biologic Properties

Bisaminoethanethiol (BAT) ligands with various gem-dimethyl and amide groups were prepared, and the corresponding neutral Tc-99m complexes were prepared and evaluated for their relative stabilities by ligand-exchange reactions. It was demonstrated that technetium complexes containing gem-dimethyl substituents have higher lipophilicities, whereas those with an amide group possess greater stability, which enhances ligand-exchange reaction. The most interesting observation was that the brain uptake in rats is not determined only by lipophilicity. Apparently, Tc-99m complexes with an amide functional group display lower brain uptakes in rats compared to those without an amide group. The brain uptake was strongly influenced by substituents on the BAT ligand. These factors are critically important and should be taken into consideration when designing Tc-99m-labeled agents for CNS receptor imaging.

1998-02-01

British Library Electronic Table of Contents (United Kingdom)

Abstract Copper(II) bis(thiosemicarbazone) are very useful for blood flow and hypoxic imaging. The aim of this study was to identify structure-activity relationships (SARs) within a series of analogues with different substitution patterns in the ligands, in order to design improved hypoxia imaging agents and elucidate hypoxia selectivity mechanisms. Genetic algorithms (GAs) were used to develop specific copper metal-ligand force field parameters for the MM3 force-field calculations. These new parameters produced results in good agreement with experiment and previously reported copper metal-ligand parameters. A successful quantitative SAR (QSAR) for predicting the several classes of Cu(II)-chelating ligands was built using a training set of 21 Cu(II) complexes. The QSAR exhibited a correlat...

2010-01-01

Orphan GPCR research

Correlations of /sup 195/Pt-/sup 31/P coupling constants with platinum-ligand and platinum-platinum bond lengths in platinum(I) dimers and in related platinum(II) complexes

Orphan G protein-coupled receptors (GPCRs) are receptors lacking endogenous ligands. Found by molecular biological analyses, they became the roots of reverse pharmacology, in which receptors are attempted...Full Text Available

2008-03-01

Complex formation of the At(I) cation with ligands containing donor atoms of the 5th, 6th and 7th main group of the periodic system

The availability of dimeric Pt(I) complexes with bridging bis(diphenylphosphino)methane ligands, (L--L')/sup n+/, presents an opportunity to study the physical properties and reactivity of metal-metal bonds as a function of the ligand trans to it with a minimum of competing variables. Several interesting trends of Pt-P coupling constants with the Pt-L and Pt-Pt bond lengths in Pt(I) dimers, (L--L')/sup n+/, and structurally related Pt(II) complexes are reported here. The data indicate that the Pt-P coupling constants continue to be sensitive indicators of not only the structure and stereochemistry of platinum phosphine complexes but also the electronic and steric influences of the ligand in such complexes, 23 references, 1 figure, 4 tables.

1986-03-12

Carbohydrate-specified endocytosis: localization of ligand in the lysosomal compartment.

Published in summary form only.

1991-11-01

Bioengineered bugs expressing oligosaccharide receptor mimics

Carbohydrate-directed endocytosis is mediated by a receptor, the hepatic binding protein; it is responsible for the clearance of galactose-terminated glycoproteins from the circulation. This process...Full Text Available

1981-11-01

Use of the 2-Pyridinealdoxime/N,N?-Donor Ligand Combination in Cobalt(III) Chemistry: Synthesis and Characterization of Two Cationic Mononuclear Cobalt(III) Complexes

Many microbial pathogens recognize oligosaccharides displayed on the surface of host cells as receptors for toxins and adhesins. These ligand-receptor interactions are critical for disease pathogenesis,...Full Text Available

2010-05-01

Thorium different-ligand complexes with morin as analytic form for extraction-photometric determination of thorium microamounts

The use of 2-pyridinealdoxime (paoH)/N,N′-donor ligand (L-L) “blend” in cobalt chemistry has afforded two cationic mononuclear cobalt(III) complexes of the general type [Co(pao)₂(L-L)]⁺,...Full Text Available

2010-01-01

Study of complexing reactions and ligand exchange of zirconium and hafnium tetrachlorides with substituted derivative of O-naphthoquinonediazide

Consideration is given to results of investigation into thorium complexing with morin (H_2Mor) in extraction systems containing different carboxylic acids as well as different salt background. The obtained data enabled to suggest the method of photometric determination of thorium in the form of Th(HMor)_2Benz_2 different-ligand complex (where Benz-anion of benzilic acid) with 0.25 #mu#g/ml detection limit.

1989-01-01

Study of complexing reactions and ligand exchange of zirconium and hafnium tetrachlorides with substituted derivative of O-naphthoquinonediazide

Using the PMR method the interaction of zirconium and hafnium tetrachlorides with tri.tet.butylphenyl ester of 1,2- naphthoquinonediazide (2)-5-sulfonic acid is studied. The formation of MCl/sub 4/xNQD complexes is established, the equilibrium constants and thermodynamic parameters of complexing reaction are determined. The presence of rapid ligand exchange, proceeding according to associative mechanism, is detected. The rate constants and activation energies of the exchange reaction are calculated.

1981-11-01

Molecules with polymerizable ligands as precursors to porous doped materials

Using the PMR method the interaction of zirconium and hafnium tetrachlorides with tri.tet.butylphenyl ester of 1,2- naphthoquinonediazide (2)-5-sulfonic acid is studied. The formation of MCl_4xNQD complexes is established, the equilibrium constants and thermodynamic parameters of complexing reaction are determined. The presence of rapid ligand exchange, proceeding according to associative mechanism, is detected. The rate constants and activation energies of the exchange reaction are calculated.

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Environmentally-Induced Malignancies: An In Vivo Model to Evaluate the Health Impact of Chemicals in Mixed Waste

Titanium and aluminum alkoxide derivatives with polymerizable ligands such as 2-(methacryloyloxy)ethylacetoacetate (HAAEMA), oleic acid and geraniol (HOGE) have been obtained. The various compounds have been characterized by FT-IR and NMR {sup 1}H. Copolymerization with styrene and divinylbenzene affords porous doped organic materials which have been characterized by scanning electron microscopy (SEM), elemental analysis, density measurements.

1996-12-31

Sorption of arsenite and arsenate on ferrihydrite: Effect of organic and inorganic ligands

Occupational and environmental exposure to organic ligands, solvents, fuel hydrocarbons, and polychlorinated biphenyls are linked with increased risk of hematologic malignancies. DOE facilities and waste sites in the U.S. are contaminated with mixtures of potentially hazardous chemicals such as metals, organic ligands, solvents, fuel hydrocarbons, polychlorinated biphenyls and radioactive isotopes. A major goal of this project was to establish linkage between chemical/radiation exposure and induction of genomic damage in target populations with the capability to undergo transformation.

2001-05-04

British Library Electronic Table of Contents (United Kingdom)

We studied the sorption of As(III) and As(V) onto ferrihydrite as affected by pH, nature and concentration of organic [oxalic (OX), malic (MAL), tartaric (TAR), and citric (CIT) acid] and inorganic [phosphate (PO4), sulphate (SO4), selenate (SeO4) and selenite (SeO3)] ligands, and the sequence of anion addition. The sorption capacity of As(III) was greater than that of As(V) in the range of pH 4.0-11.0. The capability of organic and inorganic ligands in preventing As sorption follows the sequence: SeO4~SO43 PO4. The efficiency of most of the competing ligands in preventing As(III) and As(V) sorption increased by decreasing pH, but PO4 whose efficiency increased by increasing pH. In acidic systems all the competing ligands inhibited the sorption of As(III) more than As(V), but in alkaline e...

2011-01-01

Synthesis characterization and biological evaluation of a novel mixed ligand "9"9"mTc complex as potential brain imaging agent

Presentation of Type B Peptide-MHC Complexes from Hen Egg White Lysozyme by TLR Ligands and Type I IFNs Independent of H2-DM Regulation.

One approach in the design of neutral oxotechnetium complexes is based on the simultaneous substitution of a tridentate dianionic ligand and a monodentate monoanionic coligand on a [Tc(V)O]"+"3 precursor. Following this ''mixed ligand'' concept, a novel "9"9"mTc complex with N,N-bis(2-mercaptoethyl)-N'N'-diethylethylenediamine as ligand and 1-octanethiol as coligand is prepared and evaluated as potential brain radiopharmaceutical. Preparation of the complex at tracer level was accomplished by using "9"9"mTc-glucoheptonate as precursor. The substitution was optimized and a coligand/ligand ratio of 5 was selected. Under this conditions the labeling yield was over 80% and a major product (with radiochemical purity > 80%) was isolated by HPLC methods and used for biological evaluation. Chemical characterization at carrier level was developed using the corresponding rhenium complex as structural model. ...

1998-08-01

Low concentrations of primaquine inhibit degradation but not receptor-mediated endocytosis of asialoorosomucoid by HepG2 cells

In APCs, presentation by MHC II molecules of the chemically dominant peptide from the protein hen egg white lysozyme (HEL) generates different conformational isomers of the peptide-MHC II complexes (pMHC). Type B pMHCs are formed in early endosomes from exogenous peptides in the absence of H2-DM, whereas in contrast, type A pMHC complexes are formed from HEL protein in late vesicles after editing by H2-DM. Thus, H2-DM edits off the more unstable pMHC complexes, which are not presented from HEL. In this study, we show that type B pMHC complexes were presented from HEL protein only after stimulation of dendritic cells (DC) with TLR ligands or type I IFN. Type I IFN contributed to most TLR ligand-induced type B pMHC generation, as presentation decreased in DC lacking the receptor for type I IFNs (IFNAR1(-/-)). In contrast, presentation of type A pMHC from HEL and from peptide was minimally affected by TLR ligands. The relative ...

2011-07-25

Low concentrations of primaquine inhibit degradation but not receptor-mediated endocytosis of asialoorosomucoid by HepG2 cells

Asialoorosomucoid (ASOR) is internalized and degraded by HepG2 cells after binding to the asialoglycoprotein (ASGP) receptor, internalization through the coated pit/coated vesicle pathway, and trafficking to lysosomes. Primaquine, an 8-aminoquinoline antimalarial compound, inhibits ASOR degradation at concentrations greater than 0.2 mM by neutralizing intracellular acid compartments. This leads to alterations in surface receptor number, receptor-ligand dissociation, and receptor recycling. We have investigated the effects of primaquine on 125I-ASOR uptake and degradation as a function of primaquine concentration and duration of exposure. Concentrations below those required for neutralization of acidic compartments block 125I-ASOR degradation in HepG2 cells and lead to intracellular ligand accumulation. This effect is maximal at 80 microM primaquine. The intracellular 125I-ASOR is undegraded, dissociated from the ASGP receptor, and contained ...

1991-02-01

The Notch ligand Delta-like 1 integrates inputs from TGFbeta/Activin and Wnt pathways

British Library Electronic Table of Contents (United Kingdom)

Unlike the well-characterized nuclear function of the Notch intracellular domain, it has been difficult to identify a nuclear role for the ligands of Notch. Here we provide evidence for the nuclear function of the Notch ligand Delta-like 1 in colon cancer (CC) cells exposed to butyrate. We demonstrate that the intracellular domain of Delta-like 1 (Dll1icd) augments the activity of Wnt signaling-dependent reporters and that of the promoter of the connective tissue growth factor (CTGF) gene. Data suggest that Dll1icd upregulates CTGF promoter activity through both direct and indirect mechanisms. The direct mechanism is supported by co-immunoprecipitation of endogenous Smad2/3 proteins and Dll1 and by chromatin immunoprecipitation analyses that revealed the occupancy of Dll1icd on CTGF promot...

2011-01-01

Synthesis and luminescence of Eu"3"+ and Tb"3"+ complexes with novel calix[4]arene ligands carrying 2,2'-bipyridine subunits

Complexation of nitrogen and sulphur donor Schiff's base ligand to Cr(III) and Ni(II) metal ions: Synthesis, spectroscopic and antipathogenic studies

Eu"3"+ and Tb"3"+ complexes with novel branched calix[4]arene ligands incorporating 2,2' -bipyridine subunits functionalized in the 6- or 5,5'-positions have been synthesized and their photophysical properties investigated. High luminescence intensity was obtained for the Eu"3"+ complex of the calix[4]arene ligand carrying four 5,5' -substituted- 2,2' -bipyridines, which has high molar extinction coefficients (#epsilon#_m_a_x 39 600 M"-"1 cm"-"1) and a high luminescence quantum yield (15%). (authors). 12 refs., 2 figs., 1 tab.

1995-01-01

British Library Electronic Table of Contents (United Kingdom)

2,6-Diacetyl pyridine based ligand was synthesized by the reaction of 2,6-diacetyl pyridine with thiocarbohydrazide in presence of acetic acid. The coordination compounds with Cr(III) and Ni(II) metal ions having [Cr(L)X]X2 and [Ni(L)X]X compositions (where L=ligand and X=NO3^-, Cl^- and CH3COO^-) were synthesized and characterized by physicochemical and spectral studies. The studies like elemental analyses, molar conductance measurements, magnetic susceptibility measurements, IR, UV-Vis, NMR, mass and EPR reveal that the complexes are octahedral. The compounds were examined against the pathogenic fungal and bacterial strains like Alternaria brassicae, Aspergillus niger, Fusarium oxysporum, Xanthomonas compestris and Pseudomonas aeruginosa. A. niger causes the diseases Apergillosis and Oto...

2011-01-01

Uptake of injected 125I-ricin by rat liver in vivo. Subcellular distribution and characterization of the internalized ligand.

The photoaffinity ligand [3,5-"3H] 4-azidoclonidine. Synthesis and characterization details

Subcellular-fractionation techniques were used to characterize the endocytic pathway followed by ricin in rat liver in vivo and tentatively identify the site(s) at which the ricin interchain disulphide...Full Text Available

1992-05-15

The Anti-Inflammatory Drug Leflunomide Is an Agonist of the Aryl Hydrocarbon Receptor

[3,5-"3H] 4-Azidoclonidine 6 was prepared from [3,5-"3H] 4-aminoclonidine 4 and has emerged as a valuable tool to study the alpha-2-adrenergic receptor. (author)

2004-07-01

Synthesis and characterization of new platinum(II) complexes containing oxalate and derivatives of ethylenediamine as ligands; Sintese e caracterizacao de novos complexos de platina (II) contendo oxalato e derivados da etilenodiamina como ligantes

BackgroundThe aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor that mediates the toxicity and biological activity of dioxins and related chemicals. The...Full Text Available

Synthesis and characterization of luminescent square-planar platinum(II) complexes containing dithiolate or dithiocarbamate ligands

No abstract prepared.

2006-07-01

Structure of the Taz2 domain of p300: insights into ligand binding

The synthesis, characterization, and emission properties of a series of Pt(L{sub 2})(S-S) complexes are reported. The (L{sub 2}) ligands include 4,7-diphenyl-1,10-phenanthroline (Ph{sub 2}phen), 4,4{prime}-dimethyl-2,2{prime}-bipyridine (Me{sub 2}bpy), 1,5-cyclo-octadiene (COD), trimethyl phosphite (P(OMe){sub 3}), and the {alpha}-C-deprotonated form of 2-phenylpyridine (2-phpy). The (S-S) ligands include 1-(tert-butoxycarbonyl)-1-cyanoethylene-2,2-dithiolate (tbcda), 1-(diethoxyphosphinyl)-1-cyanoethylene-2,2-dithiolate (cpdt), cis-1,2-dicarbomethoxyethylene-1,2-dithiolate (met), and N,N-diethyldithio-carbamate (Et{sub 2}dtc). The complexes are readily synthesized by the addition of the dithiolate or thiolate ligand to Pt(L{sub 2})Cl{sub 2} except for Pt(P(OMe){sub 3}){sub 2}(met), which is prepared by the addition of 2 equiv of trimethyl phosphite to Pt(COD)(met).

1994-06-22

Structure determination and investigation on cytotoxicity of potassium dichlorido(l-prolinato)platinate(II) versus chlorido(dimethyl sulfoxide)(l-prolinato)platinum(II) complex -In vitro antitumor deactivation by Cl^-/dmso ligand exchange

CBP and its paralog p300 are histone acetyl transferases that regulate gene expression by interacting with multiple transcription factors via specialized domains. The structure...Full Text Available

2009-12-01

British Library Electronic Table of Contents (United Kingdom)

Potassium dichlorido(l-prolinato)platinate(II), K[PtCl"2(l-pro"?"H)] (1), and chlorido(dimethyl sulfoxide)(l-prolinato)platinum(II), [PtCl(l-pro"?"H)(dmso)] (2), were synthesized by ligand substitution reactions. Both complexes were characterized by ^1H, ^1^3C, and ^1^9^5Pt NMR spectroscopy, elemental analysis, and HR-ESI-MS. The molecular structures of 1 and 2 were determined by single crystal X-ray diffraction, proving bidentate coordinated l-prolinato ligand and SP-4-4 configuration of 2a. With the help of DFT calculations stability of possible isomers of 1 and 2 was studied. A considerable difference in the in vitro cytotoxicity of 1 versus 2a (exchange of one chlorido ligand by dmso) against four human cancer cell lines was found.

2011-01-01

Structural basis of ligand binding by a c-di-GMP riboswitch

Solution structure of two molecular motor domains: nonclaret disjunctional and kinesin.

The second messenger signaling molecule bis-(3′-5′)-cyclic dimeric guanosine monophosphate (c-di-GMP) regulates many processes in bacteria, including motility, pathogenesis,...Full Text Available

2009-12-01

Small and neutral Tc{sup v}O BAT, bisaminoethanethiol (N{sub 2}S{sub 2}) complexes for developing new brain imaging agents

The effects of selected ligands on the structure of the truncated heavy-chain chemomechanical motor domains of Drosophila ncd and human kinesin were compared using the technique of transient electric...Full Text Available

1995-04-01

Serum RANKL, osteoprotegerin (OPG), and RANKL/OPG ratio in nephrotic children

1998-02-01

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Quantitative Analysis of Endocytosis and Turnover of Epidermal Growth Factor (EGF) and EGF Receptor

Receptor activator of NF-kB ligand (RANKL) and osteoprotegerin (OPG) play key roles in the pathogenesis of glucocorticoid-induced osteoporosis (GIO). The aim of our study was to determine whether the...Full Text Available

2010-10-01

QSAR Studies of Copper Azamacrocycles and Thiosemicarbazones

Binding of epidermal growth factor (EGF) to the EGF receptor (EGFR) initiates signal transduction, ultimately leading to altered gene expression. Ligand-activated EGFR is also rapidly internalized...Full Text Available

2010-03-01

Partial purification and some properties of a cholinesterase from bush bean (Phaseolus vulgaris L.) roots.

Genetic algorithms (GA) were used to develop specific copper metal-ligand force field parameters for the MM3 force field, from a combination of crystallographic structures and ab initio...Full Text Available

2005-08-25

New platinum(II) complexes with diamine ligands N-alkylate of long chain containing terminal hydroxyl group; Novos complexos de platina(II) com ligantes diaminados N-alquilados de cadeia longa contendo grupo hidroxila terminal

A cholinesterase was partially purified from bush bean (Phaseolus vulgaris L.) roots by using acridinium-based ligand affinity chromatography. The procedure gave a 78-fold increase in specific activity,...Full Text Available

1978-12-01

Listeria monocytogenes Infection Induces Prosurvival Metabolic Signaling in Macrophages?

No abstract prepared.

2010-07-01

In vivo evaluation of a lead-labeled monoclonal antibody using the DOTA ligand

Host cells use metabolic signaling through the LXRα nuclear receptor to defend against Listeria monocytogenes infection. 25-Hydroxycholesterol is a natural ligand of LXRs that...Full Text Available

2011-04-01

Identification of LRRc17 as a Negative Regulator of Receptor Activator of NF-?B Ligand (RANKL)-induced Osteoclast Differentiation*S?

The aim of this study was to assess the utility of a radioimmunoconjugate containing a lead radionuclide for therapy and scintigraphy applications. The radioimmunoconjugate evaluated consisted of a bifunctional DOTA ligand and monoclonal antibody (MAb) B72.3 using athymic mice bearing LS-174T tumors, human colon carcinoma xenografts. In the studies reported here, the lead-203-DOTA complex itself was first demonstrated to have in vivo stability. MAb B72.3 was then conjugated with the DOTA ligand and labeled with "2"0"3Pb, and the immunoreactivity of B72.3 was maintained. The localization of the radioimmunoconjugate to tumor tissue and other select organs paralleled that of DOTA-"1"2"5I-B72.3, suggesting a similar metabolic pattern of the two radioimmunoconjugates. Thus, the DOTA-metal complex does not alter the behavior of the radioimmunoconjugate. Tumor localization of the "2"0"3Pb-DOTA-B72.3 conjugate was demonstrated with biodistribution ...

1998-05-01

Engineering ligand-responsive RNA controllers in yeast through the assembly of RNase III tuning modules

Osteoblasts are the primary cells responsible for bone formation. They also support osteoclast formation from bone marrow precursors in response to osteotropic factors by inducing receptor activator...Full Text Available

2009-05-29

Development of a Selective Modulator of Aryl Hydrocarbon (Ah) Receptor Activity that Exhibits Anti-Inflammatory Properties

The programming of cellular networks to achieve new biological functions depends on the development of genetic tools that link the presence of a molecular signal to gene-regulatory activity. Recently,...Full Text Available

2011-07-01

Complement Factor H-Related Proteins CFHR2 and CFHR5 Represent Novel Ligands for the Infection-Associated CRASP Proteins of Borrelia burgdorferi

The aryl hydrocarbon receptor (AHR) is a ligand-activated transcription factor that mediates the toxicity of 2,3,7,8-tetrachlorodibenzo-p-dioxin. However, the role of the AHR...Full Text Available

2010-05-17

Clinical significance of Fas and FasL protein expression in gastric carcinoma and local lymph node tissues

BackgroundOne virulence property of Borrelia burgdorferi is its resistance to innate immunity, in particular to complement-mediated killing. Serum-resistant B....Full Text Available

Chiral salicyloxazolines as auxiliaries for the asymmetric synthesis of ruthenium polypyridyl complexes.

AIM: To investigate the relation of Fas and Fas ligand (FasL) protein expression with carcinogenesis and metastasis of gastric carcinoma.METHODS: Immunohistochemistry was used to detect Fas and...Full Text Available

2010-03-14

Characterization of discrete classes of binding sites of human serum albumin by application of thermodynamic principles.

Chiral auxiliaries are promising emerging tools for the asymmetric synthesis of octahedral metal complexes. We recently introduced chiral salicyloxazolines as coordinating bidentate chiral ligands which provide excellent control over the metal-centered configuration in the course of ligand substitution reactions and can be removed afterward in an acid-induced fashion under complete retention of configuration (J. Am. Chem. Soc. 2009, 131, 9602-9603). Here reported is our detailed investigation of this sequence of reactions, affording virtually enantiopure ruthenium polypyridyl complexes. The control of the metal-centered chirality by the coordinated chiral salicyloxazolinate ligand was evaluated as a function of reaction conditions, the employed bidentate 2,2'-bipyridine and 1,10-phenanthroline ligands, and the substituent at the asymmetric 5-position of the oxazoline heterocycle. Most striking was the ...

2010-09-01

Cd36, a class B scavenger receptor, functions as a monomer to bind acetylated and oxidized low-density lipoproteins

The binding interactions of four ligands differing in acid-base properties with human serum albumin (HSA) were examined as a function of temperature. Binding to HSA decreased with increasing temperature...Full Text Available

1994-08-15

Bacterial glycolipids and analogs as antigens for CD1d-restricted NKT cells

Cd36 is a small-molecular-weight integral membrane protein expressed in a diverse, but select, range of cell types. It has an equally diverse range of ligands and physiological functions, which has...Full Text Available

2007-11-01

Bacterial Particle Endocytosis by Epithelial Cells Is Selective and Enhanced by Tumor Necrosis Factor Receptor Ligands?

The CD1 family of proteins binds self and foreign glycolipids for presentation to CD1-restricted T cells. To identify previously uncharacterized active CD1 ligands, especially those of microbial origin,...Full Text Available

2005-02-01

Application of the PM6 semi-empirical method to modeling proteins enhances docking accuracy of AutoDock

Bacterial pathogens use virulence strategies to invade epithelial barriers, but active processes of epithelial cells may also contribute to the endocytosis of microbial particles. To focus on the latter,...Full Text Available

2009-03-01

Antianxiety and antidepressant-like effects of AC-5216, a novel mitochondrial benzodiazepine receptor ligand

BackgroundMolecular docking methods are commonly used for predicting binding modes and energies of ligands to proteins. For accurate complex geometry and binding energy estimation,...Full Text Available

Albumin binding of insulins acylated with fatty acids: characterization of the ligand-protein interaction and correlation between binding affinity and timing of the insulin effect in vivo.

We investigated the ability of N-benzyl-N-ethyl-2-(7,8-dihydro-7-methyl-8-oxo-2-phenyl-9H-purin-9-yl)acetamide...Full Text Available

2004-08-01

Activated PPAR? Targets Surface and Intracellular Signals That Inhibit the Proliferation of Lung Carcinoma Cells

Albumin is a multifunctional transport protein that binds a wide variety of endogenous substances and drugs. Insulins with affinity for albumin were engineered by acylation of the epsilon-amino group...Full Text Available

1995-12-15

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A Point Mutation in a Domain of Gamma Interferon Receptor 1 Provokes Severe Immunodeficiency

Peroxisome proliferator-activated receptors (PPARs) are ligand-activated transcription factors belonging to the nuclear hormone receptor superfamily. Their discovery in the 1990s provided insights...Full Text Available

2008-01-01

The "9"9Tc"m-labelling of diamino-dithiol complexes as brain imaging agents and preliminary biodistribution

Gamma interferon (IFN-γ) and the cellular responses induced by it are essential for controlling mycobacterial infections. Most patients bearing an IFN-γ receptor ligand-binding chain...Full Text Available

2001-01-01

Syntheses and phosphorus-31 NMR studies of five-coordinate platinum(II) complexes of tris(2-(diphenylphosphino)ethyl)phosphine and monodentate phosphorus ligands

Six kinds of diamino-dithiol compounds are labelled with "9"9Tc"m by ligands exchange reaction. Their ligands exchange percentage is over 95%. The biodistribution of one of these compounds in mice shows 0.88% brain uptake after two minutes and 0.28% after 15 minutes respectively. Although the brain uptake is lower for this compound, it has longer retention in brain. So, the experiment results are valuable to the design of new brain imaging agent in the future.

Status of bismuth and lead for radioimmunoimaging and therapy

The first preparation and characterization of the platinum (II) complexes containing five phosphorus ligands are reported herein. The complexes are represented by the formulae (Pt(PP/sub 3/)(P(OR)/sub 3/)Cl/sub 2/, where R = Me or Et, and (Pt(PP/sub 3/)(PEt/sub 3/))Cl/sub 2/. The /sup 31/P spectra of the complexes are presented. 10 references, 2 tables.

1987-12-02

Stability constants of At(I)-complexes with thiourea, iodide and mixed ligands in ethanol and water

Of the radionuclides with physical properties most suited for use with monoclonal antibody for tumor imaging or therapy, few are more available or desirable than Pb-203, 212 and Bi-212. Yet no clinical studies have as yet been possible solely due to the lability in vivo of known complexes. We now report that bismuth complexes of the ligands p-SCN-Bz-DOTA and p-SCN-Bz-trans-cyclohexylDTPA are effective at protecting Bi-206 from release when linked to immunoproteins. Practicable, efficient ligand syntheses will be reported. Initial studies reveal that antibody is labeled efficiently with radiolead DOTA complexes. Preliminary studies indicate stability in vivo.

1990-08-26

Metalloid Cluster Compounds of Group 14: Bonding Properties and Subsequent Reactions

The ion mobilities of |"2"1"1At|At(I) in dependence on thiourea (tu) concentration, iodide concentration and a mixture of both ligands were measured by the electromigration method in free electrolytes. An equilibrium model was developed for the characterization of electromigration curves which permitted the calculation of stability constants and ion mobilities of the complexes |AtI|, |AtI_2|"-, |Attu|"+, |Attu_2|"+ and |AtItu| existing in these solutions. Ethanol and water served as solvents. The temperature was 298 K and the ionic strength was about 0.05 mol/dm"3. (author) 16 refs.; 2 figs.

British Library Electronic Table of Contents (United Kingdom)

Metalloid cluster compounds of group 14 of the general formulae EnRm with n > m (E = Si, Ge, Sn, Pb; R = ligand), where naked as well as ligand bound tetrel atoms are present, represent a novel class of cluster compounds in group 14 chemistry and can be seen as intermediates on the way to the elemental state. Therefore, interesting properties are expected for these compounds, which might complement results from nanotechnology. In this article, first results for germanium are discussed, together with novel build-up reactions on the way to novel materials based on metalloid cluster compounds. GRAPHICAL ABSTRACT[image omitted

2011-01-01

Investigation of chloro, sulfato and oxalato-complexes of protactinium (V) by solvent extraction technique

Electrochemical and spectroelectrochemical studies on Bis(acetylacetonate)(dimethyl sulfoxide) dioxouranium(VI) in dimethyl sulfoxide

The stability constant values of Pa(V) with some complexing ligands (chloride, sulfate and oxalate) are graphically determined using solvent extraction data. The organic phase was at constant composition of HTTA in benzene while the aqueous phase was held at constant hydrogen ion concentration and ionic strength of 3. The curve-fitting method was adopted throughout this investigation, giving the following values. The stability constants obtained are used to calculate the distribution of the different Pa (V) species in the corresponding aqueous phase (expressed in mole fraction) as a function of ligand ion concentration.

Coordination lanthanide compounds with thiosemicarbazide diacetic acid

The mechanistic aspects of electrochemical reductions of U"V"IO_2(acac)_2dmso(acac=acetylacetonate, dmso=dimethyl sulfoxide) complex with bidentate ligand(acac) in DMSO were investigated by using cyclic voltammetry, normal pulse voltammetry, and spectrophotometer equipped with an optical transparent thin layer electrode cell. It is concluded that the uranyl complexes with bidentate ligands at the equatorial plane form stable U(V) complexes by the electrochemical reduction and that their molar extinction coefficients in the visible region are very small. (J.P.N.).

1996-01-01

Coordination lanthanide compounds with thiosemicarbazide diacetic acid

A study was made on complex formation of thiosemicarbazide diacetic acid (H/sub 2/L) with neodymium (3), holmium (3) and erbium (3) in solutions and formation of complexes of metal: ligand=4:1 composition was revealed. Synthesis conditions were developed and products of LnLClxnH/sub 2/O, LnLOHxnH/sub 2/O, Na(LnL/sub 2/)xnH/sub 2/O composition were separated in crystalline state. It was shown, that H/sub 2/L behaves in these compounds as tripod ligand with O, O, N, N donor atoms.

1983-02-01

Synthesis, structure, and spectroscopic properties of ortho-metalated platinum(II) complexes

A study was made on complex formation of thiosemicarbazide diacetic acid (H_2L) with neodymium (3), holmium (3) and erbium (3) in solutions and formation of complexes of metal: ligand=4:1 composition was revealed. Synthesis conditions were developed and products of LnLClxnH_2O, LnLOHxnH_2O, Na[LnL_2]xnH_2O composition were separated in crystalline state. It was shown, that H_2L behaves in these compounds as tripod ligand with O, O, N, N donor atoms.

Photoluminescent properties of heteroleptic cyclometalated platinum(II) complexes bearing 1,3-bis(3,4-dibutoxyphenyl)propane-1,3-dionate as an ancillary ligand

The ortho-metalated Pt(II) complexes Pt(ppy)(CO)Cl (1), Pt(ptpy)(CO)Cl (2), and Pt(ppy)(Hppy)Cl (3) (where ppy and ptpy are respectively the ortho-C-deprotonated forms of 2-phenylpyridine and 2-p-tolylpyridine and Hppy is 2-phenylpyridine) have been prepared. The CO ligand is coordinated trans to the nitrogen atom of the ortho-metalated ligand and exerts a strong trans effect resulting in a relatively long Pt-N bond [2.114(19) {angstrom}]. This structure shows both the bidentate ppy ligand and the monodentate Hppy with the nitrogens of these ligands trans to each other. The UV/vis electronic absorption spectra of 1-3 have intense bands in the near-UV region ({approximately}375 nm) which have been assigned as metal to ligand charge transfer (MLCT) transitions, and higher energy bands were assigned as ligand-centered transitions. Each complex exhibits relatively ...

1995-04-26

X-ray and vibrational spectroscopy of manganese complexes relevant to the oxygen-evolving complex of photosynthesis

A new series of heteroleptic cyclometalated platinum(II) complexes Pt-1a-f was synthesized, employing 2-arylpyridine (or 1-arylisoquinoline) (HC{sup L}AMDAN-1) and 1,3-bis(3,4-dibutoxyphenyl)propane-1,3-dione (HO{sup L}AMDAO-1) for cyclometalation and as ancillary ligands, respectively, and photoluminescent properties were investigated. Focusing on red-shifted phosphorescence, C{sup L}AMDAN ligands containing pi-extended aromatics and electron-rich heterocycles were examined. All obtained complexes exhibited photoluminescence at ambient temperature, and the emission maxima ranged from green (lambda{sub PL}=518 nm) to far red (lambda{sub PL}=708 nm). The large Stokes shifts of more than 100 nm and sub-microsecond or microsecond emission lifetimes revealed that these complexes are phosphorescent emissive. The quantum yield of Pt-1 ranged from 0.02 to 0.59 at ambient temperature and decreased as the emission maximum was red-shifted. In comparison ...

2010-02-15

The p75"N"T"R tumor suppressor induces cell cycle arrest facilitating caspase mediated apoptosis in prostate tumor cells

Manganese model complexes, relevant to the oxygen-evolving complex (OEC) in photosynthesis, were studied with Mn K-edge X-ray absorption near-edge spectroscopy (XANES), Mn Kb X-ray emission spectroscopy (XES), and vibrational spectroscopy. A more detailed understanding was obtained of the influence of nuclearity, overall structure, oxidation state, and ligand environment of the Mn atoms on the spectra from these methods. This refined understanding is necessary for improving the interpretation of spectra of the OEC. Mn XANES and Kb XES were used to study a di-(mu)-oxo and a mono-(mu)-oxo di-nuclear Mn compound in the (III,III), (III,IV), and (IV,IV) oxidation states. XANES spectra show energy shifts of 0.8 - 2.2 eV for 1-electron oxidation-state changes and 0.4 - 1.8 eV for ligand-environment changes. The shifts observed for Mn XES spectra were approximately 0.21 eV for oxidation state-changes and only approximately 0.04 eV for ...

2001-05-16

Structure, physical and photophysical properties of platinum(II) complexes containing bidentate aromatic and bis(diphenylphosphino)methane as ligands

The p75 neurotrophin receptor (p75"N"T"R) is a death receptor which belongs to the tumor necrosis factor receptor super-family of membrane proteins. This study shows that p75"N"T"R retarded cell cycle progression by induced accumulation of cells in G0/G1 and a reduction in the S phase of the cell cycle. The rescue of tumor cells from cell cycle progression by a death domain deleted (#DELTA#DD) dominant-negative antagonist of p75"N"T"R showed that the death domain transduced anti-proliferative activity in a ligand-independent manner. Conversely, addition of NGF ligand rescued retardation of cell cycle progression with commensurate changes in components of the cyclin/cdk holoenzyme complex. In the absence of ligand, p75"N"T"R-dependent cell cycle arrest facilitated an increase in apoptotic nuclear fragmentation of the prostate cancer cells. Apoptosis of p75"N"T"R expressing cells occurred via the intrinsic mitochondrial ...

2006-03-24

Radiolabelled D2 agonists as prolactinoma imaging agents

This study focuses on a series of Pt{sup II}(L-L{prime})(dppm){sup n+} complexes, where dppm is bis(diphenylphosphino)methane and L-L{prime} are C(caret)C{prime} (n = 0), C(caret)N (n = 1), and N(caret)N{prime} (n = 2) aromatic ligands. Structural characteristics are reported. Structural features indicate that the Pt-C bond distance is shorter than the Pt-N bond distance in symmetrical complexes and that the Pt-P bond distance trans to N is shorter than the Pt-P bond trans to C. This is consistent with the {sup 31}P NMR spectra where the chemical shift of the P trans to C is {approximately}10 ppm less than found for P trans to N. The energy maxima of the metal-to-ligand charge-transfer band for the complexes containing various L-L{prime} ligands occur in the near-UV region of the spectrum and fall into the energy series bpy > bph > phen > 2-phpy > 2-ptpy > 2-phq > 7,9-bzq, where bpy ...

2000-05-01

Platinum(II) complexes as spectroscopic probes for biomolecules

During the past year, further studies on mAChR were conducted. These studies included verification of the difference in pituitary distribution based on ligand charge. The pituitary localization of TRB. A neutral mAChR ligand, was verified. The lack of QNB blockade of TRB uptake was tested by blockage with scopolamine, another mAChR antagonist and by testing the effect in a different strain of rat. Neither scopolamine or change of rat strain had any effect. We concluded that TRB uptake in pituitary is not a receptor-mediated process. Further studies were conducted with an additional quaternized mAChR ligand: MQNB. Pituitary localization of MQNB, like MTRB, could be blocked by pretreatment with QNB. We have tentatively concluded that permanent charge on a mAChR antagonist changes the mechanism of uptake in the pituitary. Time course studies and the effects of DES on myocardial uptake are reported. A brief report on ...

1989-08-01

One-step purification of Taq DNA polymerase using nucleotide-mimetic affinity chromatography.

The use of platinum(II) complexes as tags and probes for biomolecules is indeed advantageous for their reactivities can be selective for certain purposes through an interplay of mild reaction conditions and of the ligands bound to the platinum. The use of {sup 195}Pt NMR as a method of detecting platinum and its interactions with biomolecules was carried out with the simplest model of platinum(II) tagging to proteins. Variable-temperature {sup 195}Pt NMR spectroscopy proved useful in studying the stereodynamics of complex thioethers like methionine. The complex, Pt(trpy)Cl{sup +}, with its chromophore has a greater potential for probing proteins. It is a noninvasive and selective tag for histidine and cysteine residues on the surface of cytochrome c at pH 5. The protein derivatives obtained are separable, and the tags are easily quantitated and differentiated through the metal-to-ligand charge transfer bands which are sensitive to the ...

1990-09-21

complexes of uranyl with outer-sphere perhalate anions

The thermostable Thermus aquaticus DNA polymerase (Taq Pol) has been the key factor in transforming the initial PCR method into one with huge impact in molecular biology and biotechnology. Therefore, the development of effective affinity adsorbents for the purification of Taq Pol, as well as other DNA polymerases, attracts the attention of the enzyme manufacturers and the research laboratories. In this report we describe a simple protocol for the purification of Taq Pol from E. coli lysates, leading to enzymes of high specific activity and purity. The protocol is based on a single affinity chromatography step, featuring an immobilized ligand selected from a structure-biased combinatorial library of dNTP-mimetic synthetic ligands. The ligand library was screened for its ability to bind and purify Taq Pol from E. coli lysates. One immobilized ligand (mABSGu) of the general formula X-Trz-Y, bearing ...

2007-01-01

100

Synthesis, luminescence quantum yields, and lifetimes of trischelated ruthenium(II) mixed-ligand complexes including 3,3'-dimethy1-2,2'-bipyridyl

The IR spectra of complexes of uranyl perhalates with antipyrine (AP), hexamethylphosphorus triamide (HMPTA), dimethyl sulfoxide (DMSO), and water with the composition (UO/sub 2/L/eta/)(Ha10/sub 4/)/sub 2/, where Ha10/sub 4/ = C10/sub 4//sup -/, Bro/sub 4//sup -/, 10/sub 4//sup -/ (except for DMSO and H/sub 2/O), L is a neutral ligand, n = 4 for HMPTA and n = 5 for the remaining L, were investigated. X-ray crystallographic analysis established that the investigated perhalate complexes of uranyl with the same neutral ligands are isostructural. It was established that in the complexes studied the Ha10/sub 4//sup -/ anions are outer-sphere anions, and the value of the frequency of the antisymmetrical stretching vibration of the uranyl group does not depend on the nature of the perhalate anion. From the values obtained for ..nu../sub 3/ UO /SUP 2/2/ /sup +/, the values of the multiplicity and energy of the uranium-ligand bond ...

1986-07-01

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101

Syntheses, characterizations and structures of NO donor Schiff base ligands and nickel(II) and copper(II) complexes

New five complexes of the type of [RuL sub(3-x)(dmby) sub(x)]X sub(2)(x = 1,2,3, L = 2,2'-bipyridyl or 1,10-phenanthroline, dmby = 3,3'-dimethy1-2,2'-bipyridyl, X = halide ion) have been synthesized in order to investigate the effects of two methyl groups of dmby on the absorption and emission spectra, luminescence quantum yields, and lifetimes. Values of the radiative and nonradiative rate constants have been calculated from these data at 77K. Although the absorption and emission maxima and the lifetimes are not much affected by the dmby ligand substitution, the molar extinction coefficients and emission quantum yields are decreased compared with trischelated complexes of the parent bipyridyl or phenanthroline ligands. At 25"0C the emission yields of the complexes containing dmby decrease by 3 - 4 orders of magnitude than at 77K. Possible causes of the decrease in the quantum yields are discussed. (author).

1982-01-01

102

British Library Electronic Table of Contents (United Kingdom)

New Schiff base derivatives (L1 and L2) were prepared by the condensation of 2-hydroxy-3-methoxybenzaldehyde (o-vanillin) and 3-hydroxy-4-methoxybenzaldehyde (iso-vanillin) with 5-methylfurfurylamine. Two new complexes [Ni(L1)2] and [Cu(L1)2] have been synthesized with bidentate NO donor Schiff base ligand (L1). The Ni(II) and Cu(II) atoms in each complex are four coordinated in a square planar geometry. Schiff bases (L1 and L2) and complexes [Ni(L1)2] and [Cu(L1)2] were characterized by elemental analyses, FT-IR, UV-vis, mass and 1H, 13C NMR spectroscopies. The crystal structures of the ligand (L2) and complexes [Ni(L1)2] and [Cu(L1)2] have also been determined by using X-ray crystallographic technique.

2011-01-01

103

Stereospecific ligands and their complexes. Part VII. Synthesis, characterization and in vitro antitumoral activity of platinum(II) complexes with O,Oprime-dialkyl esters of (S,S)-ethylenediamine-N,Nprime-di-2-(4-methyl)pentanoic acid

British Library Electronic Table of Contents (United Kingdom)

Platinum(II) complexes (1-4) with bidentate N,Nprime-ligands, O,Oprime-dialkyl esters (alkyl = ethyl, n-propyl, n-butyl and n-pentyl), of (S,S)-ethylenediamine-N,Nprime-di-2-(4-methyl)pentanoic acid were synthesized and characterized by IR, 1H NMR and 13C NMR spectroscopy and elemental analysis. DFT calculations were performed for the complexes and it was found that only one diastereoisomer could be formed. Cytotoxic activity of complexes 1-4 was determined against chronic lymphocytic leukemia cells (CLL) and compared to the activity of ligand precursors L12HCl-L42HCl and corresponding palladium(II) complexes, [PdCl2L] (L = L1-L4). The complexes were found to exhibit significantly higher antitumor activities than cisplatin on CLL cells. Cytotoxic effect of platinum(II) complexes on CLL cel...

2011-01-01

104

Novel platinum(II) complexes of long chain aliphatic diamine ligands with oxalato as the leaving group: Comparative cytotoxic activity relative to chloride precursors

Ligands for the peroxisome proliferator-activated receptor-#gamma# have inhibitory effects on growth of human neuroblastoma cells in vitro

Platinum complexes play an important role in the development of anticancer drugs. Their cytotoxicity can be influenced by the nature of the leaving ligands, due to the hydrolysis reaction that occurs prior to the binding of the platinum complex to DNA. Also, non-leaving groups such as lipophilic diamines may affect cellular uptake. In this work, we describe the synthesis of platinum(II) complexes having oxalato and long chain aliphatic N-alkyl ethylenediamines as ligands. The products were characterized by elemental analyses, infrared spectroscopy and {sup 1}H, {sup 13}C and {sup 195}Pt NMR spectroscopy. Biological activity was assessed against tumor cell lines (A{sub 549}, B16-F1, B16-F10, MDA-MB-231) and non-tumor cell lines (BHK-21 and CHO). The length of the carbon chain affects the cytotoxicity and the oxalato complexes were less cytotoxic than the respective chloride-containing analogues. (author)

2010-07-01

105

Comparative crystal field study of Ni{sup 2+} energy levels in NiCl{sub 2}, NiBr{sub 2}, and NiI{sub 2} crystals

The thiazolidinedione (TZD) or glitazone class of peroxisome proliferator-activated-#gamma# (PPAR-#gamma#) ligands not only induce adipocyte differentiation and increase insulin sensitivity, but also exert growth inhibitory effects on several carcinoma cell lines in vitro as well as in vivo. In the current study the in vitro effect of four PPAR-#gamma# agonists (ciglitazone, pioglitazone, troglitazone, rosiglitazone) on the cell growth of seven human neuroblastoma cell lines (Kelly, LAN-1, LAN-5, LS, IMR-32, SK-N-SH, SH-SY5Y) was investigated. Growth rates were assessed by a colorimetric XTT-based assay kit. Expression of PPAR-#gamma# protein was examined by immunohistochemistry and Western blot analysis. All glitazones inhibited in vitro growth and viability of the human neuroblastoma cell lines in a dose-dependent manner showing considerable effects only at high concentrations (10 #mu#M and 100 #mu#M). Effectiveness of the glitazones on neuroblastoma cell growth ...

2005-09-15

106

Comparative crystal field study of Ni"2"+ energy levels in NiCl_2, NiBr_2, and NiI_2 crystals

The exchange charge model of crystal field theory has been used to analyze systematically the ground state absorption spectra of octahedrally coordinated Ni{sup 2+} ion in isostructural nickel halide crystals NiCl{sub 2}, NiBr{sub 2}, and NiI{sub 2}. The parameters of the crystal field acting on the Ni{sup 2+} ion are calculated from the available crystal structure data. The obtained energy level schemes are compared with experimental absorption spectra; a good agreement with experimental data is demonstrated. Dependencies of the crystal field invariants and covalence effects on the type of ligands are considered. It is shown numerically that the overlap effects between Ni{sup 2+} ion and ligands increase with an increase of the ligands' atomic number resulting in the following order of the degree of covalence: NiI{sub 2}>NiBr{sub 2}>NiCl{sub 2}.

2006-01-15

107

Cloning and expression of a human kidney cDNA for an /alpha//sub 2/-adrenergic receptor subtype

The exchange charge model of crystal field theory has been used to analyze systematically the ground state absorption spectra of octahedrally coordinated Ni"2"+ ion in isostructural nickel halide crystals NiCl_2, NiBr_2, and NiI_2. The parameters of the crystal field acting on the Ni"2"+ ion are calculated from the available crystal structure data. The obtained energy level schemes are compared with experimental absorption spectra; a good agreement with experimental data is demonstrated. Dependencies of the crystal field invariants and covalence effects on the type of ligands are considered. It is shown numerically that the overlap effects between Ni"2"+ ion and ligands increase with an increase of the ligands' atomic number resulting in the following order of the degree of covalence: NiI_2>NiBr_2>NiCl_2.

2006-01-15

108

Tuning the spin state of iron phthalocyanine by ligand adsorption

An /alpha//sub 2/-adrenergic receptor subtype has been cloned from a human kidney cDNA library using the gene for the human platelet /alpha//sub 2/-adrenergic receptor as a probe. The deduced amino acid sequence resembles the human platelet /alpha//sub 2/-adrenergic receptor and is consistent with the structure of other members of he family of guanine nucleotide-binding protein-coupled receptors. The cDNA was expressed in a mammalian cell line (COS-7), and the /alpha//sub 2/-adrenergic ligand (/sup 3/H)rauwolscine was bound. Competition curve analysis with a variety of adrenergic ligands suggests that this cDNA clone represents the /alpha//sub 2/B-adrenergic receptor. The gene for this receptor is on human chromosome 4, whereas the gene for the human platelet /alpha//sub 2/-adrenergic receptor (/alpha//sub 2/A) lies on chromosome 10. This ability to express the receptor in mammalian cells, free of other adrenergic receptor subtypes, should help ...

1988-09-01

109

Tissue-specific expression of Fgfr2b and Fgfr2c isoforms, Fgf10 and Fgf9 in the developing chick mandible

The future use of single-molecule magnets in applications will require the ability to control and manipulate the spin state and magnetization of the magnets by external means. There are different approaches to this control, one being the modification of the magnets by adsorption of small ligand molecules. In this paper we use iron phthalocyanine supported by an Au(111) surface as a model compound and demonstrate, using x-ray photoelectron spectroscopy and density functional theory, that the spin state of the molecule can be tuned to different values (S #approx# 0, 1/2, 1) by adsorption of ammonia, pyridine, carbon monoxide or nitric oxide on the iron ion. The interaction also leads to electronic decoupling of the iron phthalocyanine from the Au(111) support. (fast track communication)

2010-12-01

110

British Library Electronic Table of Contents (United Kingdom)

SummaryExperimental evidence has demonstrated the importance of FGF signalling in morphogenesis of the mandibular processes. FGFs transmit their signals through four tyrosine kinase transmembrane receptors (FGFRs). Alternative splicing in FGFRs including FGFR2 generates different isoforms that exhibit different ligand-specificities, exclusive tissue distributions and specific biological functions. Despite extensive information regarding the isoform-specific patterns of expression Fgfr2c and Fgfr2b during morphogenesis of many organs, a comparative analysis of these specific isoforms in the chick mandible has not been reported. To better understand the function of FGFR2 in mandibular morphogenesis, we have analysed the expression Fgfr2b, Fgfr2c and their putative ligands Fgf10 and Fgf9, in ...

2006-01-01

111

Spectrophotometric study of lanthanoid complexes with antipyrine and salicylic acid

Progress and problems in the chemistry of technetium-99m tracers

The extraction-spectrophotometric method has been used to study lanthanoid ion complexing (Pr, Nd, Ho and Er) with antipyrine (Ant) and salicylic acid (Sal). The component relationship in different-ligand compounds Ln:Aut:Sal=2:3:6 and solvate number equal to 5 are determined; molar extinction coefficients of binary and different-ligand compounds are calculated. Oscillator strengths of absorption bands corresponding to supersensitive transitions of neodymium, holmium, erbium and some most intensive praseodymium bands are calculated. The study of IR spectra of investigated compounds allows to conclude on formation of coordination bonds of the central atom with the antipyrine molecule through the oxygen of the carbonyl group as well as on carboxyl group hydrogen substitution for metal and formation of coordination bond with OH group in salicylic acid molecules.

1981-01-01

112

Palladium polypyridyl complexes: synthesis, characterization, DNA interaction and biological activity on Leishmania (L.) mexicana

The recent acceleration of effort to elucidate and explore the coordination chemistry of technetium has been prompted mainly by the need for a new generation of radiotracers in nuclear medicine, preferentially for tomograhic studies. Current approaches and their limitations in designing "9"9"mTc complexes capable of penetrating cell membranes of the target organs, and remaining there sufficiently long, are reviewed. With the predominance of Tc(V) oxo compounds, especially for brain imaging agents, new N4 and N2S2 coordinate complexes have been developed by shifting from bidentate to tetradentate ligands with a variable side chain or other adjustable reactivity. The search for myocardial imaging agents has focused on a variety of mixed ligand complexes of Tc(III) and most promising [Tc(CNR)_6]"+ complexes of Tc(I). 64 refs. (author).

113

Novel photoaffinity ligands for the GA-receptor

This paper describes the search for new potential chemotherapeutic agents based on transition metal complexes with planar ligands. In this study, palladium polypyridyl complexes were synthesized and characterized by elemental analysis, NMR, UV-VIS and IR spectroscopies. The interaction of the complexes with DNA was also investigated by spectroscopic methods. All metal-to-ligand charge transfer (MLCT) bands of the palladium polypyridyl complexes exhibited hypochromism and red shift in the presence of DNA. The binding constant and viscosity data suggested that the complexes [PdCl{sub 2}(phen)] and [PdCl{sub 2}(phendiamine)] interact with DNA by electrostatic forces. Additionally, these complexes induced an important leishmanistatic effect on L. (L.) mexicana promastigotes at the final concentration of 10 {mu}mol L{sup -1} in 48 h. (author)

2008-07-01

114

Micellized sequestered silver atoms and small silver clusters

Previous studies from this laboratory have shown that certain N-substituted phthalimides (NSPs) exhibit GA-like activity in a range of specific bioassays and that bioactive NSPs compete with ({sup 3}H)-GA{sub 4} for soluble binding sites in cucumber homogenates. As such, these compounds may prove useful in the purification and characterization of GA receptor proteins. To this end, five azido-NSPs have been synthesized and are currently being screened for biological activity and photochemical stability. Three azido-NSPs elicit {alpha}-amylase production in barley half-seeds and stimulate tissue elongation in d{sub 5} maize, lettuce, sunflower, and soybean. Further evaluations are in progress and these data as well as the utility of these compounds as photo-affinity ligands will be discussed.

1990-05-01

115

Ligand Tuning in Asymmetric Hydrovinylation of 1,3-Dienes. A Stereoselective Route to either Steroid-C20 (S) or -C20 (R) Derivatives

Pulse radiolysis was used to examine the nature of the silver species obtained when an aqueous solution containing sequestered Ag"+ ions was reduced by hydrated electrons in the presence of a surfactant macrocyclic crown ether, labeled L, and/or a maltoside surfactant. The initially formed product is the Ag"0(L) species which rapidly loses its ligand (half-life #<=#5 #mu#s) and reacts with another Ag"+(L) ion to form Ag_2"+(L). The latter species decays by a bimolecular process to form the Ag_4"2"+(L)_n species at a faster rate than its ligand free analogue. Ultimately, colloidal metallic silver, (Ag)_n, forms which is stabilized by the surfactant moieties. No long-term stability to the reduced monomolecular species could be obtained.

116

Is Gold Really Softer than Silver? HSAB Principle Revisited

1,3-Dienes derived from steroidal D-ring C17-ketones undergo Ni(II)-catalyzed hydrovinylation to give 1,2- or 1,4-addition of ethylene. Using finely tuned phosphoramidite ligands it is possible to synthesize either the C20 (R)- or the C20 (S)-derivatives without mutual contamination. The proportion of the 1,4-adduct, which is also formed stereoselectively, can be minimized by optimizing the reaction conditions. Since the two alkenes in the resultant dienes have differing steric demands for many potential reactions, and are ideally juxtaposed for further D-ring functionalization, these intermediates could be useful for the preparation of biologically important compounds such as vitamin D analogs and various antitumor steroidal glycosides.

2008-06-21

117

Type I (RI) and type II (RII) receptors for transforming growth factor-beta isoforms are expressed subsequent to transforming growth factor-beta ligands during excisional wound repair.

A detailed comparison of the softness of gold and silver has been reported in the light of hard soft acid base (HSAB) principle. Gold and silver nanoparticles in organic media (i.e., organosol) have been exploited individually to establish the principle. Sulfur and nitrogen were employed as soft and borderline donating atoms to examine the metal-ligand interactions. In this regard, thiols and amines have been considered as interacting ligands with sulfur and nitrogen donor atoms respectively. The stronger affinity of gold towards softer sulfur donor as compared to nitrogen and conversely a reasonable interaction of silver nanoparticles with both the atoms authenticate the softer nature of gold nanoparticle as compared to silver one.

2006-02-15

118

The synthesis and photophysical property of [HNEt3][Cuq2IEu(hfac)3] complex

Transforming growth factor (TGF)-beta isoforms (TGF-beta 1, -beta 2, and -beta 3) regulate cell growth and differentiation and have critical regulatory roles in the process of tissue repair and remodeling....Full Text Available

1997-01-01

119

British Library Electronic Table of Contents (United Kingdom)

A new bimetallic complex [HNEt3][Cuq2IEu(hfac)3] (q^- = 8-hydroxyquinolinato, hfac^- = hexafluoroacetylacetonate) was prepared simply with only one step and characterized. Upon excitation of the organic ligand q^-, the sensitized europium luminescence was achieved.

2011-01-01

120

The chemistry of the p-block elements with thioether, selenoether and telluroether ligands.

Synthesis, crystal structure, spectroscopic and photoluminescence studies of manganese(II), cobalt(II), cadmium(II), zinc(II) and copper(II) complexes with a pyrazole derived Schiff base ligand

The synthesis and structures of acyclic and macrocyclic thio-, seleno- and telluro-ether complexes of the metallic and metalloid elements of Groups 13-16 reported since 2000 are described. The diverse structures range from discrete monomers through to infinite 1-, 2- or 3-D polymers. The coordination chemistry in this area is quite different to familiar d-block chemistry and the underlying factors are explored. PMID:21706103

2011-06-27

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16

121

British Library Electronic Table of Contents (United Kingdom)

Varying coordination modes of the Schiff base ligand H"2L [5-methyl-1-H-pyrazole-3-carboxylic acid (1-pyridin-2-yl-ethylidene)-hydrazide] towards different metal centers are reported with the syntheses and characterization of four mononuclear Mn(II), Co(II), Cd(II) and Zn(II) complexes, [Mn(H"2L)(H"2O)"2](ClO"4)"2(MeOH) (1), [Co(H"2L)(NCS)"2] (2), [Cd(H"2L)(H"2O)"2](ClO"4)"2 (3) and [Zn(H"2L)(H"2O)"2](ClO"4)"2 (4), and a binuclear Cu(II) complex, [Cu"2(L)"2](ClO"4)"2 (5). In the complexes 1-4 the neutral ligand serves as a 3N,2O donor where the pyridine ring N, two azomethine N and two carbohydrazine oxygen atoms are coordinatively active, leaving the pyrazole-N atoms inactive. In the case of complex 5, each ligand molecule behaves as a 4N,O donor utilizing the pyridine N, one azomethine N...

2011-01-01

122

Synthesis and radiolabelling of cysteine derivatives and pharmacological behaviour of their "9"9"mTc complexes

Synthesis and characterization of new platinum(II) complexes with N-alkylated ligands of longer chain containing a hydroxyl group derivatives of 1,2-etano diamine;Sintese e caracterizacao de novos complexos de platina(II) com ligantes N-alquilados de cadeia longa contendo um grupo hidroxila derivados da 1,2-etanodiamina

Full text: HMPAO, a butane monoxime derivative of propylene amine and ECD, ethyl cysteinate dimer, are currently being used as brain imaging agents. In an effort to develop new radiopharmaceuticals for imaging brain, we have synthesized amine and imine derivatives of ethyl cysteinate with butane monoxime, optimized labelling procedure with "9"9"mTc and studied the in vivo behaviour of their "9"9"mTc complexes. Imine derivative of ethyl cysteinate with butane monoxime was synthesized by refluxing equimolar amounts of butane monoxime and ethyl cystinate in dry benzene for 3 hours. The product was purified over silica with 10% ethyl acetate in chloroform as eluent. Amine derivative was prepared by reducing the imine derivative with sodium borohydride. The ligands were characterized by NMR spectroscopy and were found to be pure. The ligands were labelled with "9"9"mTc using stannous chloride as reducing agent. The complexes were characterized by ...

1998-09-01

123

Synthesis and biodistribution of nitrido technetium-99m radiopharmaceuticals with dithiophosphinate ligands: a class of brain imaging agents

No abstract prepared.

2009-07-01

124

Synthesis and biodistribution of nitrido technetium-99m radiopharmaceuticals with dithiophosphinate ligands: a class of brain imaging agents

The symmetrical complexes [{sup 99m}Tc][TcN(R{sub 2}PS{sub 2}){sub 2}] [R = CH{sub 3}, CH{sub 2}CH{sub 3}, CH{sub 2}CH{sub 2}CH{sub 3}, CH{sub 2}(CH{sub 3}){sub 2}], and the unsymmetrical complex [{sup 99m}Tc][TcN(Me{sub 2}PS{sub 2})(Et{sub 2}PS{sub 2})] have been prepared, at tracer level, through a two-step procedure involving the preliminary formation of a prereduced technetium nitrido intermediate followed by substitution reaction onto this species by the appropriate dithiophosphinate ligand [R{sub 2}PS{sub 2}]Na. The chemical identity of the resulting complexes have been established by comparison with the corresponding {sup 99}Tc-analogs prepared, at macroscopic level, by reacting the complex [{sup 99}TcNCl{sub 4}] [n-Bu{sub 4}N] (n-Bu = n-butyl) with an excess of ligand in methanol, and characterized by elemental analyses and spectroscopic techniques. The complexes are neutral and lipophilic, and possess a square pyramidal geometry, with ...

1995-04-01

125

Structural intermediates in the assembly of taxoid-induced microtubules and GDP-tubulin double rings: time-resolved X-ray scattering.

The symmetrical complexes ["9"9"mTc][TcN(R_2PS_2)_2] [R = CH_3, CH_2CH_3, CH_2CH_2CH_3, CH_2(CH_3)_2], and the unsymmetrical complex ["9"9"mTc][TcN(Me_2PS_2)(Et_2PS_2)] have been prepared, at tracer level, through a two-step procedure involving the preliminary formation of a prereduced technetium nitrido intermediate followed by substitution reaction onto this species by the appropriate dithiophosphinate ligand [R_2PS_2]Na. The chemical identity of the resulting complexes have been established by comparison with the corresponding "9"9Tc-analogs prepared, at macroscopic level, by reacting the complex ["9"9TcNCl_4] [n-Bu_4N] (n-Bu = n-butyl) with an excess of ligand in methanol, and characterized by elemental analyses and spectroscopic techniques. The complexes are neutral and lipophilic, and possess a square pyramidal geometry, with an apical Tc N group and two dithiophosphinate ligands spanning the four positions on the ...

1995-04-01

126

Solvent extraction studies using tetracycline as a complexing agent. Pt. 12. Determination of stability constants for the complexes of uranium and tetracycline

We have studied the self-association reactions of purified GDP-liganded tubulin into double rings and taxoid-induced microtubules, employing synchrotron time-resolved x-ray solution scattering. The...Full Text Available

1996-05-01

127

Reinforcing Effects of ?-Receptor Agonists in Rats Trained to Self-Administer Cocaine

Stability constants for uranium-tetracycline complexes were determined by the method of average number of ligands, the method of limiting values, the method of two parameters and the method of weighted least squares. Solvent extraction technique was used to obtain experimental data. (author). 10 refs.; 5 figs.

1985-09-01

128

Reaction with glutathione. A possible mechanism involved in rodent brain retention of a "9"9"mTc SNS/S complex containing a pendant ester functionality

σ-Receptor (σR) antagonists have been reported to block certain effects of psychostimulant drugs. The present study examined the effects of σR ligands in rats trained to self-administer...Full Text Available

2010-02-01

129

Organic electronic conductors and precursors. Pt. 15. Novel dithiolene-nickel complexes based on benzenehexathiolate derivatives

The synthesis, characterization of M"vO([CH_3CH_2N(CH_2CH_2S)_2](p-S-Ph-COOCH_2-CH_3)) (M:"9"9"mTc: I, Re: II) is presented in this work, where a pendant ester function is attached to the monothiolate ligand. Chemical structure of I is established after chromatographic comparison with II, synthesized in macroscopic amounts. Complex II is fully characterized by classical methods of analysis showing that the compound adopts a distorted trigonal bipyramidal configuration around the metal. The two sulfur atoms of the tridentate ligand and the oxo group form the basal plane, while the remaining nitrogen atom of the tridentate ligand and the sulfur atom of the monothiolate ligand occupy the apices of the bipyramid. In vitro challenge experiments with glutathione (GSH) in neutral aqueous medium demonstrate, that I suffers nucleophilic attack by GSH and thereby transformation to a more hydrophilic daughter ...

1998-08-01

130

Modulation of Retinoic Acid Receptor-related Orphan Receptor ? and ? Activity by 7-Oxygenated Sterol Ligands*

Dithiolato-nickel complexes with multisulfur ligands derived from benzenehexathiolate have been synthesized. The properties of the monomeric and polymeric complexes have been characterized by ESR spectroscopic and magnetochemical data and by electrical conductivity measurements. The prepared complexes are paramagnetic and have characteristic absorptions between 800 and 1000 nm. (orig.).

1992-04-01

131

Modification of the photodynamic action of delta-aminolaevulinic acid (ALA) on rat pancreatoma cells by mitochondrial benzodiazepine receptor ligands.

The retinoic acid receptor-related orphan receptors α and γ (RORα (NR1F1) and RORγ (NR1F3)) are orphan nuclear receptors and perform critical roles in regulation of development,...Full Text Available

2010-02-12

132

Initial Evaluation of ¹¹C-DPA-713, a Novel TSPO PET Ligand, in Humans

We have shown that addition of exogenous delta-aminolaevulinic acid (ALA) to rat pancreatoma AR4-2J cells in culture leads to the increased production of porphobilinogen (PBG) and the accumulation of...Full Text Available

1995-02-01

133

Inflammatory mediators promote production of shed LRP1/CD91, which regulates cell signaling and cytokine expression by macrophages

Translocator protein (TSPO) is upregulated in activated microglia and thus can serve as a marker of neuroinflammation. Recently, a novel radioligand, ¹¹C-N,N-diethyl-2-[2-(4-methoxyphenyl)-5,7-dimethyl-pyrazolo[1,5-a]pyrimidin-3-yl]-acetamide...Full Text Available

2009-08-01

134

Immunohistochemical localization of low density lipoprotein receptor-related protein 1 and ?₂-Macroglobulin in retinal and choroidal tissue of proliferative retinopathies

LRP1 is a type-1 transmembrane receptor that mediates the endocytosis of diverse ligands. LRP1 β-chain proteolysis results in release of sLRP1 that is present in human plasma. In this study,...Full Text Available

2010-10-01

135

Heparin blocks /sup 125/I-calmodulin internalization by isolated rat renal brush border membrane vesicles

The immunolocalization of the low density lipoprotein receptor-related protein 1 (LRP1) and its ligand alpha 2-Macroglobulin (α₂M) was examined in tissues from human donor...Full Text Available

2010-08-01

136

Expression of a functional VEGFR-1 in tumor cells is a major determinant of anti-PlGF antibodies efficacy

/sup 125/I-Calmodulin is internalized by isolated rat renal brush border membrane vesicles (BBV) in a time, temperature and calcium dependent manner. Internalization of /sup 125/I-calmodulin into the osmotically sensitive space of BBV was distinguished from binding of the ligand to the outer BBV surface by examining the interaction of ligand and BBV at different medium osmolarities (300-1100 mosm), uptake was inversely proportional to medium osmolarity. Internalized /sup 125/I-calmodulin was intact and Western blots of solubilized BBV with /sup 125/I-calmodulin demonstrated the presence of several calmodulin-binding proteins of 143, 118, 50, 47.5, 46.5 and 35 kilodaltons which could represent potential intravesicular binding sites for the ligand. Heparin and the related glycosaminoglycan heparin sulfate both showed a dose-dependent inhibition (0.5-50 ..mu..g/ml) of /sup 125/I-calmodulin uptake by BBV, but other sulfated and ...

1986-03-05

137

Excited-state properties of platinum(II) complexes containing biphenyl as a ligand: Complexes of the type [(bph)PtL[sub 2

PlGF, one of the ligands for VEGFR-1, has been implicated in tumor angiogenesis. However, more recent studies indicate that genetic or pharmacological inhibition of PlGF signaling does not result in...Full Text Available

2011-07-12

138

Efficient preparation of 99mTc(III) '4+1' mixed-ligand complexes for peptide labeling with high specific activity

The preparation, physical properties, and photophysical properties of [Pt(bph)(C[sub 2]H[sub 5])[sub 2]S][sub 2], [Pt(bph)(CH[sub 3]CN)[sub 2

1992-07-22

139

Double-antibody solid-phase radioimmunoassay: a simplified phase-separation procedure applied to various ligands

An improved labeling procedure for peptides attached to organometallic 99mTc(III) '4+1' mixed-ligand complexes in which the radiometal is coordinated by a tripodal tetradentate chelator 2,2',2''-nitrilotriethanethiol (NS3) and a monodentate isocyanide ligand is presented. The labeling procedure was evaluated by the synthesis of [99mTc(NS3)(L2-RGD)]. The containing radiopharmaceutically interesting RGD-peptide cyclo[Arg-Gly-Asp-D-Tyr-Lys] was modified with 4-isocyanobutanoic acid (L2) as linker conjugated to N6-Lys to get the monodentate ligand L2-RGD. The structural identity of the 99mTc-conjugate was confirmed by comparison to a Re reference compound. The Tc- and Re-conjugates had matching retention times under identical HPLC conditions. The 99mTc-labeling was performed in a novel one-step procedure using the eluate of a 99Mo/99mTc generator, NS3, the isocyanide modified peptide, SnCl2, Na2EDTA, mannitol and ascorbic acid ...

2010-09-01

140

Double-antibody solid-phase radioimmunoassay: a simplified phase-separation procedure applied to various ligands

The purpose was to develop a simplified and reliable method of separating free from antibody-bound ligand using a precipitating antibody linked to a cellulose derivative. Dose-response curves and control sera were set up in parallel for various pituitary and placental polypeptides, steroid hormones, insulin, glucagon, triiodothyronine, thyroxine, angiotensin I, calcitonin, gastrin, cyclic AMP, and digoxin. After first-antibody reactions had reached equilibrium, free and bound ligand were separated using a double-antibody solid-phase system in parallel with conventional methods, including dextran-coated charcoal, double-antibody precipitation, single-antibody solid phase, organic solvents, salt precipitation, and anion-exchange resins. The effect of variations in temperature, incubation time, protein content, pH, and amount of separating material added were studied. The results showed that separation was complete within 1 hr for small ...

1980-06-01

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16

141

Differential expression of human Fas mRNA species upon peripheral blood mononuclear cell activation.

142

Crystal structures of the N-terminal kinase domain of human RSK1 bound to three different ligands: Implications for the design of RSK1 specific inhibitors

Human Fas/Apo-1 is a cell-surface protein that mediates apoptosis upon ligation with Fas ligand. The gene lies on the long arm of chromosome 10, consists of nine exons, and spans more than 26 kb of...Full Text Available

1995-09-15

143

Both the Fas Ligand and Inducible Nitric Oxide Synthase Are Needed for Control of Parasite Replication within Lesions in Mice Infected with Leishmania major whereas the Contribution of Tumor Necrosis Factor Is Minimal

The p90 ribosomal S6 kinases (RSKs) also known as MAPKAP-Ks are serine/threonine protein kinases that are activated by ERK or PDK1 and act as downstream effectors of mitogen-activated protein kinase...Full Text Available

2007-12-01

144

Binding of Ru(bpy)₂(eilatin)²⁺ to Matched and Mismatched DNA

Following infection with the protozoan parasite Leishmania major, C57BL/6 mice develop a small lesion that heals spontaneously. Resistance to infection is associated with the development...Full Text Available

2003-09-01

145

Amplified B Lymphocyte CD40 Signaling Drives Regulatory B10 Cell Expansion in Mice

The DNA-binding properties of Ru(bpy)₂(eilatin)²⁺ have been investigated to determine if the sterically expansive eilatin ligand confers specificity for destabilized single-base...Full Text Available

2008-07-21

146

A novel amphiphilic pincer palladium complex: design, preparation and self-assembling behavior.

BackgroundAberrant CD40 ligand (CD154) expression occurs on both T cells and B cells in human lupus patients, which is suggested to enhance B cell CD40 signaling and play a role...Full Text Available

147

A non-toxic ligand for voxel-based MRI analysis of plaques in AD transgenic mice

Amphiphilic pincer palladium complexes bearing hydrophilic and hydrophobic side chains on the planar NCN palladium pincer backbone were designed and prepared via the ligand introduction route. The complexes self-assembled under aqueous conditions to form vesicles with bilayer membranes containing palladium species. The catalytic activity of the vesicles in the Miyaura-Michael reaction in water was investigated. PMID:21837316

2011-08-11

148

DNA cleavage on photoexposure at the d-d band in ternary copper(II) complexes using red-light laser.

Amyloid plaques are a characteristic feature in Alzheimer’s disease (AD). A novel non-toxic contrast agent is presented, Gd-DTPA-K6Aβ1–30, which is homologous to Aβ,...Full Text Available

2008-06-01

149

Theoretical investigation on quinoline-based platinum (II) complexes as efficient singlet oxygen photosensitizers in photodynamic therapy

Ternary copper(II) complexes [Cu(L1)B](ClO4) (1, 2) and [Cu(L2)B](ClO4) (3, 4), where HL1 and HL2 are tridentate NSO- and ONO-donor Schiff bases and B is a heterocyclic base, viz. dipyrido[3,2-d:2',3'-f]quinoxaline (dpq, 1 and 3) or dipyrido[3,2-a:2',3'-c]phenazine (dppz, 2 and 4), were prepared and their DNA binding and photoinduced DNA cleavage activity studied. Complex 1, structurally characterized by single-crystal X-ray crystallography, shows an axially elongated square-pyramidal (4 + 1) coordination geometry in which the monoanionic L1 binds at the equatorial plane. The NN-donor dpq ligand exhibits an axial-equatorial binding mode. The complexes display good binding propensity to calf thymus DNA, giving a relative order 2 (NSO-dppz) > 4 (ONO-dppz) > 1 (NSO-dpq) > 3 (ONO-dpq). They cleave supercoiled pUC19 DNA to its nicked circular form when treated with 3-mercaptopropionic acid (MPA) by formation of hydroxyl radicals as the cleavage active species ...

2006-12-25

150

British Library Electronic Table of Contents (United Kingdom)

Geometry optimizations of the quinoline-based platinum (II) complexes (1-R, 2-R) and their related calculations on excited state energies, electronic absorption spectra and orbital populations have been carried out by the hybrid density functional theory (DFT) and its time-dependent approach (TD-DFT). The solvent effects on excitation energies are taken into account using the conductor-like polarizable continuum model (C-PCM). The red-shifted level of absorption bands, energy gaps between the singlet ground state (S1) and the first triplet excited state (T1) for each examined complex have been elaborated thoroughly as well. We find that the quinoline-8-thoil (ligand 2) induces much more significant red-shifted level than 8-hydroxyquinoline (ligand 1), and singlet-triplet splitting energy g...

2011-01-01

151

The development of sigma-receptor specific radiopharmaceuticals for spect imaging of human tumors

Synthesis, spectral and X-ray structural studies of a NO donor Schiff base ligand and its Ni(II) complexes

The authors have been involved for the last few years in developing high affinity sigma-receptor-specific radiopharmaceuticals for use in nuclear medicine. They recently demonstrated that sigma-1 receptors are expressed in human melanoma cells and that sigma receptors could be used as external markers for non-invasive imaging. In order to determine the presence of sigma receptors in other human tumors they have screened numerous non-small cell lung carcinoma, melanoma and breast cancer cell lines. All of these cell lines expressed high sigma receptor densities using commercially available ["3H]-(+)-pentazocine or ["3H]DTG tritiated sigma ligands. Therefore, a sigma ligand with high affinity in both sigma-1 and sigma-2 subtype pharmacological assays could be potentially useful for imaging a variety of primary and metastatic sites of various origins. The authors describe recent efforts to develop high affinity sigma radiopharmaceuticals and ...

1994-08-21

152

British Library Electronic Table of Contents (United Kingdom)

The Schiff base ligand, 4-isopropylbenzaldehyde[N-(3-oxo-3,4-dihydro-2-quinoxalinyl)hydrazone] (Ipbh), the 1:1 condensation product of 4-isopropylbenzaldehyde and 2-hydroxy-3-hydrazinoquinoxiline, has been synthesized and characterized by X-ray crystallography. A series of complexes of Ipbh with Nickel(II), viz., [Ni(Ipbh)2]Cl2 (1), [Ni(Ipbh)2]Br2 (2), [Ni(Ipbh)2]I2 (3), [Ni(Ipbh)2(CH3OH)2](NO3)2(CH3OH)2 (4) and [Ni(Ipbh)2ClO4]ClO4 (5) have been synthesized. All the complexes were characterized by elemental analysis, molar conductivity, CHN analysis, spectroscopic studies, magnetic susceptibility measurements and TG/DTA methods. The solid-state structure of the complex 4 was established by single crystal X-ray crystallography. In all the complexes, Ipbh acts as a bidentate NO chelating age...

2011-01-01

153

Synthesis, characterization and catalytic activities of vanadium complexes containing ONN donor ligand derived from 2-aminoethylpyridine

British Library Electronic Table of Contents (United Kingdom)

Reaction between [V^I^VO(acac)2] and the ONN donor Schiff base Hpydx-aepy (I) (Hpydx-aepy=Schiff base obtained by the condensation of pyridoxal and 2-aminoethylpyridine) resulted in the formation of a complex [V^I^VO(acac)(pydx-aepy)] (1). Addition of aqueous 30% H2O2 to 1 yields the poor stable oxidoperoxidovanadium(V) complex [V^VO(O2)(pydx-aepy)] (2). Its formation has also been demonstrated in solution by treating 1 with H2O2 in methanol. Reaction of vanadium exchanged zeolite-Y with I in methanol followed by aerial oxidation gave zeolite-Y encapsulated dioxidovanadium(V) complex, abbreviated as [V^VO2(pydx-aepy)]-Y (4). The crystal and molecular structure of 1 has been determined, confirming the ONN binding mode of the ligand. The encapsulated complex [V^VO2(pydx-aepy)]-Y (4) catalyse...

2011-01-01

154

Synthesis, characterization and biological evaluation of mononuclear Co(II), Ni(II), Cu(II) and Pd(II) complexes with new N2O2 Schiff base ligands.

Synthesis, characterization and antitumor activity study of some cyclometalated organoplatinum(II) complexes containing aromatic N-donor ligands

New tetradentate N(2)O(2) donor Schiff bases and their mononuclear Co(II), Ni(II), Cu(II), and Pd(II) complexes were synthesized and characterized extensively by IR, (1)H-, (13)C-NMR, mass, ESR, conductivity measurements, elemental and thermal analysis. Specifically the magnetic and electronic spectral measurements demonstrate the octahedral structures of cobalt(II), nickel(II) complexes and square planar geometries of copper(II), palladium(II) complexes. All the ligands and complexes were screened for their in vitro antibacterial activity against two gram-positive bacteria (Bacillus subtilis, Staphylococcus aureus) and two gram-negative bacteria (Escherichia coli, Klebsiella pneumonia). In this study, Pd(II) complexes exhibited potent antibacterial activity against B. subtilis, S. aureus whereas other metal complexes also exerted good activity towards all tested strains even than standard drugs streptomycin and ampicillin. PMID:21297294

2011-02-01

155

British Library Electronic Table of Contents (United Kingdom)

A general approach has been designed to synthesize some mononuclear and binuclear cyclometalated platinum(II) complexes, containing aromatic N-donor ligands with the presence of one Cl- trans to carbon. In this way, cyclometalated platinum(II) complex [Pt(C^N)Cl(dmso)], 1, C^N = N(1),C(2prime)-chelated, deprotonated 2-phenylpyridine and dmso = dimethylsulfoxide, was used as a precursor to react with imidazole derivatives (1-methylimidazole, 2a, imidazole, 2b,), monodentate pyridine derivatives (4-methylpyridine, 2c, pyridine, 2d,) and bidentate pyridine derivative (4,4prime-bipyridine, 3 and 4,). Synthesized complexes were fully characterized by using multinuclear NMR spectroscopy (1H, 13C{1H} and 195Pt), correlation NMR spectroscopy (1H-1H COSY, 13C{1H}-1H Heteronuclear Multiple Quantum C...

2011-01-01

156

Synthesis and characterization of diastereomeric (substituted iminodiacetato)(1,2-diaminocyclohexane)platinum(II) complexes

Studies on the Evolution of Silver Nanoparticles in Micelle by UV-Photoactivation

Novel complexes of the type (Pt(DACH)(N-R-iminodiacetate)), wherein DACH represents (R,S)- and (R,R)-1,2 diaminocyclohexane and R represents /minus/Me, /minus/EtOH, and /minus/CH/sub 2/Ph groups, have been prepared, purified, and characterized by spectroscopic techniques (/sup 1/H, /sup 13/C, and /sup 195/Pt NMR;MS(FAB);IR) and by the measurement of selected physical properties (pH, pK/sub a/, conductivity, and molecular weights). The data are consistent with the formation of two diastereomeric complexes in unequal proportions in which the N-R-iminodiacetate ligand appears to be bonded as a pseudofacial tridentate chelate. One are of the ligand forms a stable five-membered-ring O,N-chelate while the other arm appears to be involved in ion-pair formation (zwitterion-like) involving the carboxylate anion and the formally positive Pt(II) central metal atom. It has been demonstrated indirectly that an active impurity was present in predictably ...

1988-11-16

157

Studies on some N-acyl N-phenylhydroxylamines as metal-complexing ligands - Part IX : formation constants of UO_2"2"+-complexes of some-hydroxysuccinamic acid

Ultraviolet (UV) photoirradiation of Ag(I) compounds in the presence of an aqueous Triton X-100 solution has been exploited for the first time to prepare reproducible yellow silver hydrosol. The evolution of nanosized silver particles has been examined critically under the influence of different anions/ligands. Hence, time dependent evolution of silver hydrosol from different silver compounds in micelle via photochemical reduction is observed. Anions/ligands of precursor salts have been found to show profound influence (due to electron scavenging property, solubility, stability etc.) on the evolution route and efficiency of photochemical reduction of Ag(I) to Ag(O) in micelle and thereby classification of silver compounds becomes possible. Kinetic results reveal that the formation of silver particles proceeds via autocatalytic growth mechanism. The observed variation in rate constant values for the evolution of nanoparticles from different ...

2003-12-15

158

Spectral properties of new dioxouranium (VI) complexes with tridentate ono donor schiff bases

The first-step formation constants of UO_2"2"+-complexes of some N-hydroxysuccinamic acids viz. N-phenyl N-hydroxysuccinamic acid (Rsub(p)H(sub(2))), N-o-toyl N-hydroxysuccinamic acid(Rsub(t)oHsub(2)) and N-m-tolyl N-hydroxysuccinamic acid (Rsub(t)mHsub(2)) have been determined spectrophotometrically. Stabilities are in the ligand order Risup(m)Hsub(2)>Rsub(t)oHsub(2)>Rsub(p)Hsub(2). The first-step hydrolysis constant k' of UO_2"2"+ ion has been determined spectrophotometrically and found to be pk'=4.00 at a constant ionic strength (#mu#=0.5) at 30deg-+0.5deg and the molar extinction coefficients of the species UO_2"2"+ and UO_2(OH)"+ at #LAMBDA#=385 nm are found to be 2.0 and 13.0 respectively. (author).

1976-01-01

159

Radiolabelled D_2 agonists as prolactinoma imaging agents: Progress report for period February 1, 1988--January 31, 1989

New dioxouranium (VI) complexes of Schiff bases derived from orthaminophenol and salicylaldehyde, 5,6-benzosalicyladehyde, orthohydroxyacetophenone, orthohydroxybenzophenone, acetoacetanilide and benzoylacetanilide have been prepared and characterized by elemental analysis, conductance, molecular weight, infrared, electronic spectra and magnetic susceptibility measurements. The schiff bases behave as ONO donor tridentate dibasic ligands. Two types of complexes, viz. UO_2L.CH_3OH and UO_2L_2 (where LH_2 schiff base) have been synthesized. The comlexes are monomers, nonelectrolytes and diamagnetic. The #nu#(C=N), #nu#(C-O) (phenolic), #nu#(C-O)(CH_3OH) and the ligands. The #nu#sub(as)(O = U =0) occurs in the range 885-940 cm"-"1 and U-O bond length lies in the 1.72-1.74 A range. The 1:1 complexes are six-cordinated and 1:2 complexes are eight coordinated. (author).

1982-01-01

160

Radiolabelled D/sub 2/ agonists as prolactinoma imaging agents: Progress report for period February 1, 1988--January 31, 1989

Targeted studies completed include the evaluation of tritiated N-0437, evaluation of "3"5S-cysteamine, evaluation of "1"8F-FDG and initiation of synthetic efforts towards the synthesis of iodinated N-0437 and pergolide analogs. The direction of the project has been changed due to several factors which include the decided lack of favorable experimental results, the excellence of results using muscarinic receptor ligands in pituitary, brain and heart and the contention of the DOE review panel that the original grant proposal was based on flawed assumptions together with their perceived lack of importance to pituitary imaging. In the final year of this grant, three studies will be completed. The first study is the continuation of synthetic efforts to prepare iodinated N-0437 and pergolide analogs for possible use as brain imaging agents. The second study is directed towards completion of biochemical evaluation of various muscarinic receptor analogs for heart, brain ...

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16

161

Phenolics from Glycyrrhiza glabra roots and their PPAR-g ligand-binding activity

Targeted studies completed include the evaluation of tritiated N-0437, evaluation of /sup 35/S-cysteamine, evaluation of /sup 18/F-FDG and initiation of synthetic efforts towards the synthesis of iodinated N-0437 and pergolide analogs. The direction of the project has been changed due to several factors which include the decided lack of favorable experimental results, the excellence of results using muscarinic receptor ligands in pituitary, brain and heart and the contention of the DOE review panel that the original grant proposal was based on flawed assumptions together with their perceived lack of importance to pituitary imaging. In the final year of this grant, three studies will be completed. The first study is the continuation of synthetic efforts to prepare iodinated N-0437 and pergolide analogs for possible use as brain imaging agents. The second study is directed towards completion of biochemical evaluation of various muscarinic receptor analogs for heart, ...

1988-10-15

162

British Library Electronic Table of Contents (United Kingdom)

Bioassay-guided fractionation of the EtOH extract of licorice (Glycyrrhiza glabra roots), using a GAL-4-PPAR-g chimera assay method, resulted in the isolation of 39 phenolics, including 10 new compounds (1-10). The structures of the new compounds were determined by analysis of their spectroscopic data. Among the isolated compounds, 5prime-formylglabridin (5), (2R,3R)-3,4prime,7-trihydroxy-3prime-prenylflavane (7), echinatin, (3R)-2prime,3prime,7-trihydroxy-4prime-methoxyisoflavan, kanzonol X, kanzonol W, shinpterocarpin, licoflavanone A, glabrol, shinflavanone, gancaonin L, and glabrone all exhibited significant PPAR-g ligand-binding activity. The activity of these compounds at a sample concentration of 10mg/mL was three times more potent than that of 0.5mM troglitazone.

2010-01-01

163

New dioxomolybdenum(VI) complexes with tridentate dibasic ONO donor schiff bases

Luminescent property and catalytic activity of Ru(II) carbonyl complexes containing N, O donor of 2-hydroxy-1-naphthylideneimines

Several dioxomolybdenum(VI) complexes of the schiff bases derived from salicylaldehyde, 2-hydroxy-1-naphthaldehyde, o-hydroxyacetophenone or pyridoxal and o-aminobenzylalcohol, o-aminophenol, o-hydroxybenzylamine, o-hydroxy(methylbenzyl)amine or 3-amino-2-naphthoic acid have been synthesized and characterized by elemental analysis, electrical conductance, molecular weight, IR and electronic spectral and magnetic susceptibility measurements. The schiff bases behave as dibasic, tridentate ligands and coordinate through ONO donor system forming complexes of the type MoO_2L.X (where LH_2=schiff base, X=H_2O or Ch_3OH). The compounds MoO_2L.Ch_3OH react with 2,2'-dipyridyl to form heterochelates of the type MoO_2L.dipyridyl. The complexes are non-electrolytes, monomers, diamagnetic and possess a cis-MoO_2 structure. The complexes exhibit a ligand-to-metal charge-transfer transition around 25000 cm"-"1. The complexes MoO_2L.X and MoO_2L.dipyridyl are ...

164

British Library Electronic Table of Contents (United Kingdom)

The reaction of the chelating ligands (obtained by the condensation of 2-hydroxy-1-naphthaldehyde with various primary amines) with [RuHCl(CO)(EPh3)2(B)] (where E=P; B=PPh3, py or pip: E=As; B=AsPh3) in benzene afforded new stable ruthenium(II) carbonyl complexes of the general formula [Ru(Cl)(CO)(EPh3)(B)(L)] (L=anion of bidentate Schiff bases). The structure of the new complexes was investigated using elemental analyses, spectral (FT-IR, UV-vis and 1H NMR) and electrochemical studies and is found to be octahedral. All the metal complexes exhibit characteristic MLCT absorption and luminescence bands in the visible region. The luminescence efficiency of the ruthenium(II) complexes was explained based on the ligand environment around the metal ion. These complexes catalyze oxidation of prim...

2007-01-01

165

Interpreting the visible absorption bands of 1,4-(dihydroxy)-9,10-anthraquinone and its metal chelates.

Immunolocalization of endothelin-B receptor in mouse intestinal tract.

The visible absorption spectra of 1,4-(dihydroxy)-9,10-anthraquinone and of Co(II), Ni(II), Cu(II) and Zn(II) chelates have been studied in different organic solvents. This system provides a model for the anthracycline antibiotics and their metal chelates. The band structure of the spectrum has been determined using the second and fourth derivatives of the spectrum. The visible absorption band of the parent molecule can be assigned to a single electronic state with a reduced dipole moment in the excited state; structure in this band is ascribed to two overlapping vibrational progressions. In contrast, the dianion (hydroxy protons removed) shows a single electronic state with an increased dipole moment in the excited state; structure in this band can be assigned to a single vibrational progression. All of the metal chelates show spectra which are similar in appearance to that of the dianion although the identity of the metal determines the bathochromic shift of the absorption band. ...

1990-08-15

166

Human complement protein C99 is a calcium binding protein

The endothelin-B (ETB) receptor is a G-protein-coupled receptor that binds endothelin ligands and is essential for the development of epidermal melanocytes and enteric neurons. Recent reports indicate that ETB is localized to nuclei in cardiac ventricular myocytes, although it has been thought that ETB is localized mainly on the plasma membrane. It remains unknown, however, whether this unique distribution of ETB occurs in other tissues. To elucidate the subcellular distribution of ETB in the intestine, we performed immunofluorescence of ETB in mouse intestine using a specific antibody. ETB-like immunoreactivity was detected in both the mucosal and muscle layers. In the mucosal layer, villous epithelial cells, stromal cells of the lamina propria, and cryptic cells were immunostained. Subcellularly, ETB is localized mainly to the nuclei of villous epithelial cells. In the muscle layer, immunoreactivity of ETB was localized to the myenteric plexus. These findings ...

2004-11-01

167

Electronic absorption and emission spectra of Alq3 in solution with special attention to a delayed fluorescence

Human complement protein C9 is shown to be a metalloprotein that binds 1 mol of Ca"2"+/mol of C9 with a dissociation constant of 3 #mu#m as measured by equilibrium dialysis. Incubation with EDTA removes the bound calcium, resulting in a apoprotein with decreased thermal stability. This loss in stability leads to aggregation and, therefore, to loss of hemolytic activity upon heating to a few degrees above the physiological temperature. Heat-induced aggregation of apoC9 can be prevented by salts that stabilize proteins according to the Hofmeister series of lyotropic ions, suggesting that the ion in native C9 may ligand with more than one structural element of domain of the protein. Ligand blotting indicates that the calcium binding site is located in the amino-terminal half of the protein. Removal of calcium by inclusion of EDTA in assay mixtures has no effect on the hemolytic activity of C9, and its capacity to bind to C8 in solution, or to ...

168

Diaqua[N,Nprime-(o-phenylene)bis(pyridine-2-carboxamidato)-k4N]manganes e(III) perchlorate

Tris(8-quinolinolato)aluminum(III) (Alq3) shows electronic absorption bands at 378, 360 (in a 1:1 mixed solvent of methanol and ethanol (ME) at 77 K), 334, 316, 300, 263, 255.8, and 233 nm in ethanol at room temperature. According to the polarized fluorescence excitation spectrum together with MO calculations, for instance, the 360 nm band is assigned to an LL CT transition (an intramolecular charge transfer transition between two ligands), and the 378 nm band to an LM/ML CT one (an intramolecular charge transfer transition between ligand and metal). Alq3 shows a broad fluorescence band peaking at around 478 nm in the ME matrix at 77 K. The emission spectrum measured with a phosphoroscope has two emission bands at 567 and 478 nm. The 567 nm band accompanies vibronic bands at 578 and 605 nm, being safely assigned to a phosphorescence of Alq3. The lifetimes of the 478 and 567 nm bands are both 5.4 ms. The lifetime of the 478 nm band together with ...

2008-08-01

169

British Library Electronic Table of Contents (United Kingdom)

In the MnIII complex of the title compound, [MnIII(C18H12N4O2)(H2O)2]ClO4, the MnIII atom is coordinated by four N atoms from the bpb2- [1,2-bis(pyridine-2-carboxamido)benzene] ligand located in the equatorial plane and two O atoms of water molecules at axial positions, yielding a distorted MnN4O2 octahedral coordination geometry. The bpb2- ligand is nearly planar, with a maximum deviation of 0.2311 (3) A from the mean plane. The MnIII complex cation and the perchlorate anion, both of which are located on twofold rotation axes, are connected by O-H...O and C-H...O hydrogen bonds into a three-dimensional supramolecular network structure.

2007-01-01

170

Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor

Cyclopalladated 2-phenyldihydrooxazole complexes with ethylenediamine, 2,2?-bipyridine, and bridging acetate ligands

Crystallography and computer modeling have been used to exploit a previously unexplored channel in the glucocorticoid receptor (GR). Highly potent, nonsteroidal indazole amides showing excellent complementarity to the channel were designed with the assistance of the computational technique AlleGrow. The accuracy of the design process was demonstrated through crystallographic structural determination of the GR ligand-binding domain-agonist complex of the D-prolinamide derivative 11. The utility of the channel was further exemplified through the design of a potent phenylindazole in which structural motifs, seen to interact with the traditional GR ligand pocket, were abandoned and replaced by interactions within the new channel. Occupation of the channel was confirmed with a second GR crystal structure of this truncated D-alaninamide derivative 13. Compound 11 displays properties compatible with development as an intranasal solution formulation, ...

2010-09-17

171

British Library Electronic Table of Contents (United Kingdom)

The 1H NMR, electronic absorption, and luminescence spectra, as well as voltammograms of the reduction and oxidation of the complexes [Pd(C?N)(N?N)]ClO4 and [Pd(C?N)(?-OOCCH3)]2 [where (C?N)? is deprotonated 2-phenyl-4,5-dihydro-1,3-oxazole, and N?N is ethylenediamine or 2,2?-bipyridine (bpy)] were compared. Magnetic nonequivalence of protons in the dihydrooxazole ring and upfield shift of the corresponding signals were observed as a result of anisotropic effect of the ring current in palladated phenyl substituents in the [Pd(C?N)(?-OOCCH3)]2 complex having a C 2 symmetry. One-electron reduction wave of [Pd(C?N)bpy]+ was assigned to ligand-centered electron transfer to the ?* orbital of 2,2?-bipyridine, and two oxidation waves of [Pd(C?N)(?-OOCCH3)]2 were attributed to successive one-elect...

2011-01-01

172

Bis(acetylacetonato)ruthenium Complexes of Noninnocent 1,2-Dioxolene Ligands: Qualitatively Different Bonding in Relation to Monoimino and Diimino Analogues

British Library Electronic Table of Contents (United Kingdom)

Abstract Coordination compounds [Ru(acac)2(Q)] (acac=acetylacetonate; Q=o-benzoquinone) were prepared as complexes 1 (Q=o-benzoquinone), 2 (Q=3-methoxy-o-benzoquinone), 3 (Q=4-methyl-o-benzoquinone), and 4 (Q=3,5-di-tert-butyl-o-benzoquinone). The structures of 1 and 2 were determined to reveal a RuIII/o-benzosemiquinone formulation, supported by analysis of experimental data (spectroscopy, magnetism of 1) and by DFT calculations. The S=1 ground state calculated for 1 stands in contrast to the spin-paired analogues with arylimino-o-benzosemiquinonato and diimino-o-benzoquinone ligands. The close contacts of about 5.3- possible between semiquinone O atoms of different molecules in the crystal allow for intermolecular spin-spin interactions and an overall complex magnetic behavior. One quasi...

2011-01-01

173

Binary copper(II) and uranyl(VI) complexes of glycocyamine, taurine and pyridoxal and ternary complexes involving 2,2'-bipyridine, 1,10-phenanthroline or nitrilotriacetic acid

A joint computational and experimental study of a novel dioxomolybdenum(VI) complex bearing chiral N,N-dimethyllactamide ligand

Chelating tendencies of several biologically important compounds viz. glycocyamine (GCN: N-amidino-aminoethanoic acid) taurine (TRN: 2-aminoethanesulphonic acid) and pyridoxal [PDL: 3-hydroxy-5-(hydroxymethyl)-2-methyl-pyridine-4-carbaldehyde] have been examined by pH-metric titration technique in their binary complex formation with copper(II) and uranyl(VI) ions. The work has further been extended to investigating the ternary complex formation involving 2.2'-bipyridine. 1,10-phenanthroline or nitrilotriacetic acid as a primary and TRN and PDL as secondary ligands. All the experiments were carried out at 25"0C and at an ionic strength of 0.1M (NaCl0_4) in aqueous or 50% (v/v) aqueous-ethanol medium according to the suitability of the experimental conditions. Stabilities of ternary complexes as compared to those of the corresponding binary complexes of the secondary ligands have also been discussed. (author).

174

British Library Electronic Table of Contents (United Kingdom)

A new cis-dioxomolybdenum complex MoO2(DMLA)2 (DMLA=N,N-dimethyllactamide) has been synthesized and characterized by X-ray crystallography, H NMR and IR spectroscopies and electronic structure calculations at DFT/B3LYP level. This compound (chemical formula C10H20MoO6N2) crystallizes in the orthorhombic space group P212121 with Z=4, a=6.9357(2)?, b=11.8761(4)?, c=17.7251(5), V=1460.00(8)?3 and renders a slightly distorted octahedral structure with two long Mo-O bonds (2.253(3)? and 2.257(3)?) trans to each of the MoO groups and with two short Mo-O bonds of 1.942(3)4? cis to them. The MoO bond length are 1.715(3) and 1.704(3)?). Each lactamide ligand is bidentate; they are coordinated in their deprotonated form with the carbonyl oxygen occupy...

2011-01-01

175

"2"1"1At-Rh(16-S4-diol) complex as a precursor for astatine radiopharmaceuticals

Tetrakis (. mu. -pyrophosphito) diplatinum (II) Tetraanion. A potential inorganic material for the fabrication of luminescent solar concentrators

"2"1"1At is one of the most promising radionuclides in #alpha#-radioimmunotherapy (#alpha#-RIT). Unfortunately, biomolecules labeled by direct electrophilic astatination are unstable due to the rapid loss of "2"1"1At under both in vitro and in vivo conditions. The present paper describes the results of our studies on attaching At"- to the rhodium(III) complex with thioether ligand: 1,5,9,13-etrathiacyclohexadecane-3,11-diol (16-S4-diol). Rh"3"+ was chosen as a moderately soft metal cation which should form very strong bonds with soft At"- anions, but first of all because of the kinetic inertness of low spin rhodium(III) d"6 complexes. The 16-S4-diol ligand was selected due to formation of stable complexes with Rh"3"+. The experiments related to optimization of the reaction conditions were performed with the "1"3"1I, basing on a chemical similarity of I"- to At"-. The experiments with "2"1"1At were then carried out under the conditions found ...

176

Synthesis and characterization of nickel(II), chromium(III), cobalt(II), copper(II), zinc(II), and cadmium(II) complexes with isatin- isonicotinoylhydrazone

In this note it is suggested that binuclear platinum(II) complexes with a solely inorganic bridging pyrophosphito ligand also possess many of the complementary advantages of inorganic and organic dyes. They are evaluated for their potential use as a luminescent solar concentrator material. The disadvantages include: the high cost of platinum; the absorption spectra in solution shows a weaker absorption at 452 nm which may cause reabsorption of emitted light; the positions of the absorption and emission maxima are not at the optimal wavelengths for absorption of sunlight and emission to a solar cell. In spite of these drawbacks the author believes the platinum complexes merit consideration for fabrication of solar concentrator devices.

1986-01-01

177

Solution-based characterization of surface-enhanced Raman response of single scattering centers

A few metal complexes of isatin-isonicotinoylhydrazone with Ni(II), Cr(III), Co(II), Cu(II), Zn(II) and Cd(II) have been prepared and characterized on the basis of elemental analyses, infrared and electronic spectra as well as "1H NMR spectra, conductivity and magnetic measurements. In view of the results obtained, it has been found that two molecules of isatin-isonicotinoylhydrazone are chelated to the central metal ion as bis-uninegative ONO tridentate ligand forming non-electrolytic octahedral metal complexes. (author)

1997-03-01

178

Solid-phase synthesis and pharmacological evaluation of novel nucleoside-tethered dinuclear platinum(II) complexes

We demonstrate the rapid optical characterization of large numbers of individual metal nanoparticles freely diffusing in colloidal solution by confocal laser spectroscopy. We find that hollow gold nanospheres and solid silver nanoparticles linked with a bifunctional ligand, both designed nanostructures, exhibit significantly higher monodispersity in their Rayleigh and Raman scattering response than randomly aggregated gold and silver nanoparticles. We show that measurements of rotational diffusion timescales allow sizing of particles significantly more reliably than can be obtained using translational diffusion timescales.

2008-03-06

179

British Library Electronic Table of Contents (United Kingdom)

Three novel inosine-based dinuclear platinum complexes have been synthesized via a solid-phase strategy. In these compounds, the metal is linked both to the N-7 of the purine nucleus and to the terminal amine group of a hexylamine side chain installed on N-1. Cis- or trans- diamine as well as ethylenediamine ligands are coordinated to platinum along with a chloride. The synthesised complexes were tested against four different human tumor cell lines. One of these complexes proved to be more cytotoxic than cisplatin against the MCF7 cancer cell line in a short-term exposure assay.

2011-01-01

180

Magnetic properties of CeRh_2Si_2 and CePd_2Si_2 single crystals

Lanthanide(III) complexes of ONO donor schiff bases derived from salicylaldehyde and o-hydroxybenzylamine or o-aminobenzylalcohol

Single-crystalline CeRh_2Si_2 and CePd_2Si_2 were grown by the Czochralsky pulling method and the temperature dependence of magnetic susceptibility was investigated. The crystalline electric field (CEF) states in each compound were determined by considering the tetragonal CEF Hamiltonian with mean-field approximation. Interactions between Ce"3"+ ion and the surrounding ligands in CeRh_2Si_2 turned out to be strong and highly anisotropic in comparison to CePd_2Si_2. (orig.)

1998-01-01

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16

181

Disruption of contact inhibition in rat liver epithelial cells by various types of AhR ligands

Several new complexes of isomeric schiff bases derived from salicylaldehyde and o-hydroxybenzylamine/o-aminobenzyl-alcohol with Pr(III), Nd(III), Sm(III), Gd(III), Tb(III), and Dy(III) have been synthesized and characterized by elemental analysis, molar conductance, IR, electronic spectra and magnetic susceptibility measurements. The schiff bases behave as monobasic tridentate ONO donor and dibasic tridentate ONO donor ligands and form complexes of the type Ln(LH)L. (author). 12 refs.

1988-01-01

182

Synthesis, characterization, and evaluation of a novel bifunctional chelating agent for the lead isotopes {sup 203}Pb and {sup 212}Pb

The maintenance of a balance between cell gain and cell loss is essential for proper liver function. The exact role of aryl hydrocarbon receptor (AhR) in regulating cell proliferation and apoptosis of liver cells remains unclear, since ligand-dependent activation of AhR has been shown to induce cell cycle arrest, proliferation, differentiation or apoptosis, depending on the cellular model used. AhR can directly interact with retinoblastoma protein in hepatic cells, forming protein complexes that can efficiently block cell cycle progression by inducing G1 arrest, or to induce the expression of inhibitors of cyclin-dependent kinases, such as p271. On the other hand, it has been suggested that AhR could play a stimulatory role in cell proliferation, either directly or by mediating a release from contact inhibition. It is now generally accepted that progenitor cells exist in the liver, are activated in various liver diseases and can form a potential target cell ...

2004-09-15

183

Synthesis, characterization, and evaluation of a novel bifunctional chelating agent for the lead isotopes "2"0"3Pb and "2"1"2Pb

Radioisotopes of Pb(II) have been of some interest in radioimmunotherapy and radioimmunoimaging (RII). However, the absence of a kinetically stable bifunctional chelating agent for Pb(II) has hampered its use for these applications. {sup 203}Pb (T{sub 1/2}=52.02 h) has application potential in RII, with a {gamma}-emission that is ideal for single photon emission computerized tomography, whereas {sup 212}Pb (T{sub 1/2}=10 h) is a source of highly cytotoxic {alpha}-particles via its decay to its {sup 212}Bi (T{sub 1/2}=60 min) daughter. The synthesis of the novel bifunctional chelating agent 2-(4-isothiocyanotobenzyl)-1,4,7,10-tetraaza-1,4,7,10-tetra-(2-carbamoyl methyl)-cyclododecane (4-NCS-Bz-TCMC) is reported herein. The Pb[TCMC]{sup 2+} complex was less labile to metal ion release than Pb[DOTA]{sup 2-} at pH 3.5 and below in isotopic exchange experiments. In addition to increased stability to Pb{sup 2+} ion release at low pH, the bifunctional TCMC ligand was ...

2000-01-01

184

Structural Investigations of Silica Polyamine Composites: Surface Coverage, Metal Ion Coordination, and Ligand Modification

Radioisotopes of Pb(II) have been of some interest in radioimmunotherapy and radioimmunoimaging (RII). However, the absence of a kinetically stable bifunctional chelating agent for Pb(II) has hampered its use for these applications. "2"0"3Pb (T_1_/_2=52.02 h) has application potential in RII, with a #gamma#-emission that is ideal for single photon emission computerized tomography, whereas "2"1"2Pb (T_1_/_2=10 h) is a source of highly cytotoxic #alpha#-particles via its decay to its "2"1"2Bi (T_1_/_2=60 min) daughter. The synthesis of the novel bifunctional chelating agent 2-(4-isothiocyanotobenzyl)-1,4,7,10-tetraaza-1,4,7,10-tetra-(2-carbamoyl methyl)-cyclododecane (4-NCS-Bz-TCMC) is reported herein. The Pb[TCMC]"2"+ complex was less labile to metal ion release than Pb[DOTA]"2"- at pH 3.5 and below in isotopic exchange experiments. In addition to increased stability to Pb"2"+ ion release at low pH, the bifunctional TCMC ligand was found to have many other ...

2000-01-01

185

Structural Investigations of Silica Polyamine Composites: Surface Coverage, Metal Ion Coordination, and Ligand Modification

Silanization of the silica gel surface in the synthesis of silica gel polyamine composites uses (chloropropyl)-trichlorosilane (CPTCS). It is possible to substitute a molar fraction of reagent CPTCS with methyltrichlorosilane (MTCS), creating a mixed silane surface layer. Two types of silica gels were modified with a series of MTCS:CPTCS molar ratios. Solid-state CP/MAS 29Si and 13C NMR spectroscopies were used to evaluate the surface silane composition. Surface silane coverage was markedly improved for the resulting gels. When polyamines were grafted to the resultant MTCS:CPTCS silane layers, it was shown that the decrease in the number of propyl attachments to the polyamine resulted in increased quantities of ''free amines''. Optimum MTCS:CPTCS ratios were determined for three polyamines grafted onto one silica gel. A substantial free amine increase was observed for poly(allylamine) (PAA). Metal uptake studies show increases in Cu(II) capacity ...

2006-09-13

186

Kinetic, spectroscopic and chemical modification study of iron release from transferrin; iron(III) complexation to adenosine triphosphate

2006-09-13

187

Comparison of angiotensin II and SAR1, Ile8-AII binding to solubilized receptors in the bovine adrenal

Amino acids other than those that serve as ligands have been found to influence the chemical properties of transferrin iron. The catalytic ability of pyrophosphate to mediate transferrin iron release to a terminal acceptor is largely quenched by modification non-liganded histine groups on the protein. The first order rate constants of iron release for several partially histidine modified protein samples were measured. A statistical method was employed to establish that one non-liganded histidine per metal binding domain was responsible for the reduction in rate constant. These results imply that the iron mediated chelator, pyrophosphate, binds directly to a histidine residue on the protein during the iron release process. EPR spectroscopic results are consistent with this interpretation. Kinetic and amino acid sequence studies of ovotransferrin and lactoferrin, in addition to human serum transferrin, have allowed the ...

1985-01-01

188

Azathia crown ethers carrying pyrene pendant as receptor molecules for metal sensor systems

Derivatives of angiotensin with a sarcosine substitution at the carboxy terminus and an aliphatic amino acid substitution at the amino terminus have been shown to be competitive ligands for the angiotensin receptor. Scatchard plots derived from saturation isotherm data in bovine adrenal particulates consistently demonstrate three to five times the number of binding sites for "1"2"5I-Sarl,Ile8-AII ("1"2"5I-SI-AII) than for "1"2"5I-AII in experiments in which the two ligands are run side-by-side. A significant difference between "1"2"5I-AII and "1"2"5I-SI-AII binding to detergent solubilized angiotensin receptors was observed. Of the "1"2"5I-AII binding sites, about 85-90% were recovered upon solubilization. In contrast, the recovery of "1"2"5I-SI-AII binding sites was only 4-5%. To determine whether binding sites labeled in the soluble state represent biologically significant AII receptors, they examined the ability of selected angiotensin ...

1986-04-13

189

A zwitterionic silylene as reactive intermediate and its unusual dimerization to an N-heterobicyclic disilane.

A series of crown ethers carrying a pyrene group with nitrogen-sulfur donor atoms, that differ in having three, four and five sulfur atoms in the macrocycle was designed and synthesized by the reaction of the corresponding macrocyclic compound and 1-bromomethylpyrene. The influence of metal cations such as Mn2+, Fe2+, Fe3+, Co2+, Ni2+, Cu2+, Zn2+, Cd2+, Hg2+, Pb2+ and Al3+ on the spectroscopic properties of the ligands was investigated in acetonitrile-dichloromethane (1:1) by means of absorption and emission spectrometry. Absorption spectra show isosbestic points in the spectrophotometric titration of Fe2+, Zn2+, Cu2+, Pb2+ and Hg2+. The results of spectrophotometric titration experiments disclosed the complexation compositions and complex stability constants of the novel ligands with Fe2+, Zn2+, Cu2+, Pb2+ and Hg2+ cations. The monoazatetrathia crown ether showed good sensitivity for Cu2+ with linearity in the range 5.0x10-7-2.5x10-6 M and ...

2011-04-01

190

In vitro and in vivo evaluation of novel ligands for radioimmunotherapy

A way to synthesize the transient zwitterionic silylene L'Si: 8 {L'=CH[(C=CH(2))CMe(N(tBu))(2)]} and achieve its facile dimerization to the remarkable N-heterobicyclic disilane 8(2) is described. At first, employing the beta-diketiminate ligand L [L=CH(CMeN(tBu))(2)], both starting materials LH (2) and its N-lithium salt LLi (3) can react with SiBr(4) to yield the silylene precursor L'SiBr(2) (4) by silicon-induced C-H activation at an exocyclic methyl group on the backbone of the ligand. Compound 4 reacts with SiBr(4) above room temperature to afford the unexpected terminal CH(SiBr(3))-substituted dibromosilane 6 along with the unique tricyclic trisilane 7. Reduction of 4 with KC(8) at 0 degrees C furnishes the novel N-heterobicyclic disilane 8(2), which is a formal dimer of the desired zwitterionic silylene L'Si: (8). It has been reasoned that compound 8(2) may results from [4+1] cycloaddition of two molecules of 8 to give the transient dimer ...

2009-08-01

191

Heterodifunctional ligands derived from monooxidized Bis(phosphino)amines. Synthesis and transition metal (Molybdenum(0), Tungsten(0), Rhodium(I), Palladium(II), and Platinum(II)) complexes of (Diphenylphosphino)(diphenylphosphinothioyl)- and (Diphenylphosphino) (diphenylphosphinoselenoyl)phenylamine, Ph[sub 2]PN(Ph)P(E)PH[sub 2] (E = S, Se). Crystal and molecular structure of the Pt(II) Complex [Cl[sub 2]P[ovr tPPh[sub 2]N(Ph)P(S)]Ph[sub 2

Novel ligands cis-2,6-bis[N,N-bis(carboxymethyl)aminomethyl]-1-piperidineacetic acid (PIP-DTPA), cis-[(1R,11S)-6,9,15-Tris-carboxymethyl-3,6,9,15-tetraazabicyclo[9.3.1] pentadec-3-yl]-acetic acid (PIP-DOTA), cis-{l_brace}2,7-bis-[bis-carboxymethyl-amino)-methyl]-azepan-1-yl{r_brace}-acetic acid (AZEP-DTPA), [2-(4,7-bis-carboxymethyl-[1,4,7]triazacyclononan-1-yl-ethyl] -2-carbonylmethyl-amino]-tetraacetic acid (NETA) and [{l_brace}4-carboxymethyl-7-[2-(carboxymethylamino)-ethyl]-perhydro-1,4,7-triazonin-1-yl{r_brace}-acetic acid (NPTA) are investigated as potential chelators of {sup 177}Lu, {sup 9}Y, {sup 212}Pb and {sup 213}Bi for radioimmunotherapy (RIT). The new ligands are radiolabeled with {sup 177}Lu, {sup 86/88/9}Y, {sup 203}Pb and {sup 205/6}Bi, and in vitro stability and in vivo stability of the radiolabeled complexes are assessed in human serum and athymic mice, respectively. In vitro studies indicate that all radiolabeled complexes ...

2006-05-15

192

The contribution of lower vertebrate animal models in human reproduction research

Bis(diphenylphosphino)phenylamine can be selectivity oxidized by S or Se in toluene or hexane solvents to the monooxidized thioyl or selenoyl products Ph[sub 2]PN(PH)PPh[sub 2]=E, (E = S, Se). These compounds act as bidentate chelate ligands toward metal complexes forming (CO)[sub 4]M(LL) (M = Mo, W), CO(Cl)Rh(LL), and Cl[sub 2]M(LL), (M = Pt, Pd) where (LL) is the thioyl or selenoyl derivative of the aminobis(phosphine). IR and NMR data are given for all complexes. The carbonyl infrared stretching frequencies show that the chelates form with the phosphine cis to any CO which is present. The [sup 31]P NMR of all complexes of two doublets except for the Rh complexes wherein the Rh spin also couples to phosphorous to produce two doublets of doublets. The [sup 2]J[sub PP] values range from 56 to 112 Hz. [sup 1]J[sub PSe] coupling provide valuable assistance for the assignment of the phosphorus resonances which range widely from 55 to 126 ppm for P[sup III] and from 60 ...

1993-12-08

193

British Library Electronic Table of Contents (United Kingdom)

Many advances have been carried out on the estrogens, GnRH and endocannabinoid system that have impact in the reproductive field. Indeed, estrogens, the generally accepted female hormones, have performed an unsuspected role in male sexual functions thanks to studies on non-mammalian vertebrates. Similarly, these animal models have provided important contributions to the identification of several GnRH ligand and receptor variants and their possible involvement in sexual behavior and gonadal function regulation. Moreover, the use of non-mammalian animal models has contributed to a better comprehension about the endocannabinoid system action in several mammalian reproductive events. We wish to highlight here how non-mammalian vertebrate animal model research contributes to advancements with i...

2011-01-01

194

The N-terminal domain of a-dystroglycan, released as a 38kDa protein, is increased in cerebrospinal fluid in patients with Lyme neuroborreliosis

British Library Electronic Table of Contents (United Kingdom)

a-Dystroglycan is an extracellular adhesion protein that is known to interact with different ligands. The interaction is thought to stabilize the integrity of the plasma membrane. The N-terminal part of a-dystroglycan may be proteolytically processed to generate a small 38kDa protein (a-DG-N). The physiological significance of a-DG-N is unclear but has been suggested to be involved in nerve regeneration and myelination and to function as a potential biomarker for neurodegenerative and neuromuscular diseases. In this report we show that a-DG-N is released into different body fluids, such as lachrimal fluid, cerebrospinal fluid (CSF), urine and plasma. To investigate the significance of a-DG-N in CSF we examined the levels of a-DG-N and known neurodegenerative markers in CSF from patients di...

2011-01-01

195

Targeting the nicotinic alpha7 acetylcholine receptor to enhance cognition in disease

British Library Electronic Table of Contents (United Kingdom)

A promising drug target currently under investigation to improve cognitive deficits in neuropsychiatric and neurological disorders is the neuronal nicotinic alpha7 acetylcholine receptor (a7nAChR). Improving cognitive impairments in diseases such as Alzheimer's (AD) and schizophrenia remains a large unmet medical need, and the a7nAChR has many properties that make it an attractive therapeutic target. The a7nAChR is a ligand gated ion channel that has particularly high permeability to Ca^2^+ and is expressed in key brain regions involved in cognitive processes (e.g., hippocampus). The a7nAChRs are localized both pre-synaptically, where they can regulate neurotransmitter release, and post-synaptically where they can activate intracellular signaling cascades and influence downstream processes...

2011-01-01

196

Synthesis, Characterization and Biological Properties of Anions of Bivalent Transition Metal [Co(II) and Ni(II)] Complexes With Acylhydrazine Derived ONO Donor Schiff Bases.

Synthesis and biodistribution of "9"9"mTc-peptides conjugated adenine as tumor imaging agents

Some acylhydrazine derived ONO donor Schiff bases and their Co(II) and Ni(II) complexes have been prepared having the same metal ion (cation) but different anions. These synthesized metal(II) complexes have been characterized on the basis of their elemental analyses, magnetic moment, molar conductance, and IR and electronic spectral data. All of the Schiff base ligands function as tridentates and the deprotonated enolic form is preferred for coordination. In order to evaluate the effect of anions on the bactericidal activity, these synthesized complexes, in comparison to the uncomplexed Schiff bases have been screened against bacterial species., Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa and the results are reported. PMID:18475936

2000-01-01

197

Surface oxidation of Co2+ and its dependence on ligand coordination number in silica polyamine composites

Two peptide ligands conjugated adenine, [9-N-(tritylmercapto acetyl diglycyl aminoethyl) adenine, Tr-MAG_2-Ade] and [9-N-(tritylmercapto acetyl triglycyl aminoethyl) adenine, Tr-MAG3-Ade], are synthesized and labeled with "9"9"mTc by directly labeling method. The stability of "9"9"mTc-MAG_2- adenine and "9"9"mTc-MAG_3-adenine in vitro is measured. The uptake radios of tumor to muscle at 3h post-injection are 5.70 and 4.92, respectively. The biodistribution and scintigraphic imaging studies show that the two complexes have high localization in tumor and high contrasted tumor images can be obtained, which suggest their potential utility as tumor imaging agents. But the high radioactivity of abdomen could prevent the tumor imaging in this area. (author)

2007-07-01

198

British Library Electronic Table of Contents (United Kingdom)

Coordination of CoCl2 solutions to the silica polyamine composite, WP-1, made with the branched polymer polyethylenimine (PEI) shows irreversible binding resulting from surface oxidation of the Co2+-Co3+. This is not the case for the silica polyamine composite BP-1 made with the linear polymer polyallylamine where reversible binding and no oxidation is observed. These observations suggested that oxidation of the cobalt was related to the greater coordination number available with the branched polyamine relative to the linear polyamine. A study of the kinetics of cobalt binding to WP-1 indicated initial loading of Co2+ at relatively low coordination number followed by desorption of Co2+ leading to oxidation and irreversible binding. Exclusion of oxygen from the composite-cobalt solution mix...

2010-01-01

199

Role of Fgf receptor 2c in adipocyte hypertrophy in mesenteric white adipose tissue

British Library Electronic Table of Contents (United Kingdom)

Fgf receptor 2c (Fgfr2c) was expressed in mature adipocytes of mouse white adipose tissue (WAT). To examine the role of Fgfr2c in mature adipocytes, we generated adipocyte-specific Fgfr2 knockout (Fgfr2 CKO) mice. The hypertrophy impairment of adipocytes in the mesenteric WAT but not in the subcutaneous WAT and decreased plasma free fatty acid (FFA) levels were observed in Fgfr2 CKO mice. Although the expression of genes involved in adipocyte differentiation and lipid metabolism in the mesenteric WAT was essentially unchanged, the expression of uncoupling protein 2 potentially involved in energy dissipation was significantly increased. Among potential Fgf ligands for Fgfr2c, Fgf9 was preferentially expressed in the mesenteric WAT. The present findings indicate that Fgfr2c potentially activ...

2008-01-01

200

Resonance Raman and photophysical studies of transition metal complexes in solution and entrapped in zeolites

Quantification of Free and Bound Fractions of Nickel in Natural Waters by Solvent Extraction with 1,2-Cyclohexanedione Bis-Benzoyl-Hydrazone

We have obtained convincing evidence for localization of the optical electron on a single-ring fragment of a chelated bipyridine-like'' ligand (ie., pyridylpyrazine or 4-Methyl-bipyridine). In addition we have completed studies of Ru(bipyrazine){sub 3}{sup 2+} in aqueous sulfuric acid (0--98% by weight) and find clear evidence for sequential addition of six-protons to the six peripheral nitrogen atoms. Studies of zeolite-entrapped complexes are continuing and a series of homo- and heteroleptic complexes have been prepared and characterized. Finally, the synthesis of zeolite-entrapped metallophthalocyanines has now been developed and the copper and cobalt analogues synthesized. The characterization of these materials is now in progress.

1992-03-31

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16

201

British Library Electronic Table of Contents (United Kingdom)

An hydrazone derivative, 1,2-cyclohexanedione bis-benzoyl-hydrazone (1,2-CHBBH), has been used as a selective reagent for an advanced environmental application consisting of separating the different species of nickel in natural waters by solvent extraction. The effects of pH and reagent concentration on the extraction process were studied, as well as the influence of both organic (humic acids) and inorganic ligands (Cl-). Under natural conditions, organic and inorganic nickel species presented different extraction behaviors, and the variations in extraction yields could be correlated with the concentrations of organic complexes in the samples, allowing the separation of labile and non-labile nickel species in both fresh and marine waters.

2010-01-01

202

Pseudohalogen compounds of astatine: synthesis and characterization of At(I)-tricyanomethanide-and At(I)-azide-compounds

NIR-emissive erbium-quinolinolate complexes

Reactions of At(#THETA#)"+, 'At"0.H_2O', AtCl_2"- and AtBr_2 with the pseudohalogenides tricyanomethanide and azide are described. Information on the compound formation of astatine with C(CN)_3"- and N_3"- could be obtained on the basis of electromigration investigations under variation of the conditions (composition of the electrolyte, pH, exchange reactions of ligands). Astatine(I)-tricyanomethanide is classified between AtI_2"- and At(SCN)_2"-. The formation of astatine(I)-azide-compounds is confirmed. Their composition is probably At(N_3)_2"-. There is no dependence of the ion mobility of astatine(I)-azide in the investigated range on azide concentration which is due to its high stability. (author).

203

British Library Electronic Table of Contents (United Kingdom)

Studies addressed to a deep understanding of the structure/property relationship on the near infrared (NIR)-emissive erbium-quinolinolate complexes, which are of interest for low-cost photonic systems, are reviewed. The role of the 8-quinolinolate ligand (Q), which studies also as sensitizer to overcome the weak absorptivity of lanthanide ion, is discussed. Synthetic and structural aspects are reported to revise the old assumption that these complexes are analogous in structure to AlQ3 and to point out the specificity of the lanthanide coordination chemistry. In fact depending on reaction conditions, species with high coordination numbers and differing for nuclearity and stoichiometry have been isolated and fully characterized. In some instances it has been shown that coordinated water mol...

2011-01-01

204

Metal ion complexation by ionizable crown ethers

Mechanical Properties of Nanocrystal Supercrystals

Research conducted since the last progress report includes the synthesis and characterization of twenty three novel proton-ionizable crown ether compounds. Metal ion complexation behavior of new and previously-synthesized proton-ionizable crown ether compounds has been probed by solvent extraction and transport across polymer-supported liquid membranes. The behavior of neutral polyether and proton-ionizable polyether ligands in polymeric membrane electrodes has been assessed. Studies of the use of proton-ionizable crown ethers for separation of lithium isotopes were initiated. Also, the thermodynamics of interactions between alkali metal cations and ionized crown ethers have been probed by titration calorimetry. 10 refs., 1 tab.

1989-09-01

205

Magnetic properties of CeRh{sub 2}Si{sub 2} and CePd{sub 2}Si{sub 2} single crystals

Colloidal nanocrystals attract significant interest due to their potential applications in electronic, magnetic, and optical devices. Nanocrystal supercrystals (NCSCs) are particularly appealing for their well ordered structure and homogeneity. The interactions between organic ligands that passivate the inorganic nanocrystal cores critically influence their self-organization into supercrystals, By investigating the mechanical properties of supercrystals, we can directly characterize the particle-particle interactions in a well-defined geometry, and gain insight into both the self-assembly process and the potential applications of nanocrystal supercrystals. Here we report nanoindentation studies of well ordered lead-sulfide (Pbs) nanocrystal supercrystals. Their modulus and hardness were found to be similar to soft polymers at 1.7 GPa and 70 MPa respectively and the fractures toughness was 39 KPa/m1/2, revealing the extremely brittle nature of these materials.

2009-12-30

206

In vitro and in vivo evaluation of [{sup 123}I]-VEGF{sub 165} as a potential tumor marker

Single-crystalline CeRh{sub 2}Si{sub 2} and CePd{sub 2}Si{sub 2} were grown by the Czochralsky pulling method and the temperature dependence of magnetic susceptibility was investigated. The crystalline electric field (CEF) states in each compound were determined by considering the tetragonal CEF Hamiltonian with mean-field approximation. Interactions between Ce{sup 3+} ion and the surrounding ligands in CeRh{sub 2}Si{sub 2} turned out to be strong and highly anisotropic in comparison to CePd{sub 2}Si{sub 2}. (orig.) 10 refs.

1998-01-01

207

Human and rat mast cell high-affinity immunoglobulin E receptors: Characterization of putative. alpha. -chain gene products

One of the research challenges in oncology is to develop new biochemical methods for noninvasive tumor therapy evaluation to determine whether the chemotherapeutics is effective. Vascular endothelial growth factor (VEGF) was labeled with radioiodine and evaluated in vitro as well as in vivo, using A2058, a melanoma cell line overexpressing VEGFR-1 and -2. Saturation binding analysis with [{sup 125}I]-VEGF resulted in a K {sub d} of 0.1 nM. Internalization assays indicate the preserved ligand induced internalization and metabolization of the tracer. Biodistribution studies with [{sup 123}I]-VEGF in wild type and A2058 tumor-bearing athymic mice showed low background activity and a tumor to reference tissue ratio of maximum 6.12. These results suggest that [{sup 123}I]-VEGF is a potentially suitable tracer for tumor therapy evaluation.

2005-07-01

208

Homogeneous models for mechanisms of surface reactions: Propylene ammoxidation

The authors have cloned and determined the entire nucleotide sequence of cDNAs corresponding to the putative {alpha} subunits of the human and rat mast cell high-affinity IgE receptors. Both human and rat cDNAs encode an NH{sub 2}-terminal signal peptide, two immunoglobulin-like extracellular domains (encoded by discrete exons), a hydrophobic transmembrane region, and a positively charged cytoplasmic tail. The human and rat {alpha} subunits share an overall homology with one another and the immunoglobulin gene family, suggesting that they arose from a common ancestral gene and continue to share structural homology with their ligands. In addition, the rat gene is transcribed into at least three distinct forms, each of which yields a somewhat different coding sequence.

1988-03-01

209

Growth of ytterbium tartrate trihydrate crystals in silica and agar-agar gels and their characterization

The proposed active sites on the catalyst surface in heterogeneous propylene ammoxidation have been successfully modelled by structurally characterized pinacolato W(VI) tert-butylimido complexes. These compounds exist as an equilibrating mixture of amine-bis(imido) and imido-bis(amido) complexes, the position of this equilibrium is dependent on the electronic nature of the glycolate ligand. Both of the C-N bond-forming reactions proposed in recent studies by Grasselli et al. (1) have been reproduced using discrete Group VI d{sup 0} organoimido complexes under mild conditions suitable for detailed mechanistic studies. These reactions are: (1) oxidative trapping of radicals at molybdenum imido sites, and (2) migration of the allyl group from oxygen to an imido nitrogen atom.

1987-04-01

210

British Library Electronic Table of Contents (United Kingdom)

Single crystals of ytterbium tartrate trihydrate have been grown by gel method using silica and agar-agar gels as media of growth. The medium of growth influences the morphology of grown crystals, silica gel yielding single and polycrystalline in the form of spherulites whereas agar-agar gel leading to growth of single and twinned crystals. Materials grown as single crystals have been characterized by using optical and scanning electron microscopy (SEM), EDAX, XRD, FT-IR, CHN and thermogravimetric techniques. The stoichiometry of the grown single crystals is suggested to be Yb(C4H4O6) (C4H5O6).3H2O. The FT-IR spectrum shows the presence of singly as well as doubly ionized tartrate ligands. Results of thermal analysis indicate that the material is thermally stable up to a temperature of 200...

2006-01-01

211

Gadolinium (III) chelates of O, N-donor Schiff bases derived from 2, 3-dimethyl-4-formyl-1-phenyl-3-pyrazoline-5-one and certain aromatic amines

Energy transfer study of europium-tetracycline complexes

New Schiff base chelating ligands were synthesized by reacting equimolar quantities of 2,3-dimethyl-4-formyl-1-phenyl-3-pyrazoline-5-one and o-anisidine, p-anisidine, m-anisidine, o-toluidine, p-toluidine, m-toluidine, 2,6-xylidine or 2,4-xylidine in ethanol medium. Their subsequent reaction with gadolinium (III) nitrate hexahydrate in 2:1 molar ratio gave complexes that were characterized by elemental analyses, molar conductances, magnetic measurements, electronic and I.R. spectral studies. All the chelates were found to be non-electrolytic in nature. (author). 15 refs., 1 fig., 1 tab.

1994-01-01

212

Electronic structures of organometallic complexes of f elements. XLIV. Parametrization of the crystal field splitting pattern of [(MeCp)_3PrCl]"-

The aim of this work was to study the energy transfer mechanisms from the ligand to the central lanthanide ion of tetracycline-europium (Tc-Eu) complex. The absorption spectra of a EuCl{sub 3}.H{sub 2}O solution was measured and absorption cross-section of Eu{sup 3+} was estimated. The observed overlap predicts a resonant energy transfer from Tetracycline to Eu{sup 3+}. The microscopic parameter of energy transfer was obtained using the overlap integral calculation considering a dipole-dipole energy transfer mechanism and results were compared considering an energy transfer by exchange. In this work, we report also the optical properties of Tc-Eu complex when urea hydrogen peroxide is added to the aqueous solution.

2007-01-15

213

Dosimetry of iodine-123 iomazenil in humans

The absorption and magnetic circular dichroism spectra of [N(n-Bu)_4]"+[(MeCp)_3PrCl]"- dissolved in 2-MeTHF were measured at room and at low temperatures. On the basis of these spectra the crystal field splitting pattern could be derived. The parameters of an empirical Hamiltonian were fitted to the energies of 42 levels to give an r.m.s. deviation of 23 cm"-"1. From the crystal field parameters obtained the crystal field strength of the ligand collective was estimated. Compared with neutral Cp_3Pr circle B complexes the crystal field strength of the anionic [(MeCp)_3PrCl]"- moiety is unusually low. (orig.)

1998-07-24

214

Direct nano ESI time-of-flight mass spectrometric investigations on lanthanide BTP complexes in the extraction-relevant diluent 1-octanol

The distribution of the central benzodiazepine receptor specific ligand iodine-123 iomazenil was investigated in seven human adults from whole-body scans, blood samples and urine collected up to 24 h after injection. Using 12 source organs, the MIRD method was applied to calculate the absorbed radiation dose of the radioligand in various organs. The urinary bladder wall (0.15 mGy/MBq), lower large intestinal wall (0.071 mGy/MBq) testes (0.044 mGy/MBq) and upper large intestined wall (0.038 mGy/MBq) received the highest absorbed doses. The average effective dose equivalent of "1"2"3I-IBZM for adults was estimated to be 0.033 mSv/MBq. (orig.).

215

Dielectric properties of sols of silver nanoparticles capped by alkyl carboxylate ligands

The present work focuses on investigations of a highly selective ligand for Am(III)/Ln(III) separation: bis-triazinyl-pyridine (BTP). By means of nano-electro-spray mass spectrometry, complex formation of BTP with selected elements of the lanthanide series is investigated. We show that the diluent drastically influences complex speciation. Measurements obtained in the extraction-relevant diluent 1-octanol show the occurrence of Ln(BTP){sub i} (i 1-3) species in different relative abundances, depending on the lanthanide used. Here, the relative abundances of the Ln(BTP){sub 3} complexes correlate with the distribution ratios for extraction to the organic phase of the respective lanthanide. (authors)

2009-12-15

216

British Library Electronic Table of Contents (United Kingdom)

Sols of silver nanoparticles in toluene were studied by broadband dielectric spectroscopy (10?3?105 Hz). The frequency dependences of the specific alternating current (ac) conductivity and the complex electric modulus were used to estimate the temperature/frequency intervals of long- and short-range charge transfer occurs, respectively. A considerable increase (by more than 30 ?C) in the Vogel temperature T 0 and the glass transition temperature T g in sols compared with the pure solvent was found. It can be hypothesized that these cooperative effects reflect the initial stage of the superlattice formation. Although the dielectric characteristics of sols are generally controlled by the conductivity relaxation, the dielectric response was observed in the high-frequency range (1?103 Hz) at l...

2011-01-01

217

Determination of platinum and ruthenium in Pt and Pt-Ru catalysts with carbon support by direct and derivative spectrophotometry.

Constrained NBMPR analogue synthesis, pharmacophore mapping and 3D-QSAR modeling of equilibrative nucleoside transporter 1 (ENT1) inhibitory activity

Platinum and ruthenium in carbon supported Pt and Pt-Ru catalysts were determined by direct and derivative spectrophotometric methods. Complexes of platinum and ruthenium with SnCl(3)(-) ligands (tin(II) chloride in HCl) were used to determine both metals in solutions obtained after digestion of the samples of the catalysts. Platinum in the Pt/C catalyst can be determined in solutions obtained by digestion of the samples in aqua regia. Derivative spectrophotometry was used to determine both metals in the presence of each other in solutions obtained after digestion of samples of the Pt-Ru/C catalyst in the mixture of HCl+HNO(3) (6:1). The first derivative at 377 nm (;zero-crossing' point of ruthenium) and the second-derivative values at 495 nm (;zero-crossing' point of platinum) were used to estimate the concentration of platinum and ruthenium, respectively. PMID:18967441

1999-01-01

218

British Library Electronic Table of Contents (United Kingdom)

Conformationally constrained analogue synthesis was undertaken to aid in pharmacophore mapping and 3D-QSAR analysis of nitrobenzylmercaptopurine riboside (NBMPR) congeners as equilibriative nucleoside transporter 1 (ENT1) inhibitors. In our previous study [J. Med. Chem. 2003, 46, 831-837], novel regioisomeric nitro-1,2,3,4-tetrahydroisoquinoline conformationally constrained analogues of NBMPR were synthesized and evaluated as ENT1 ligands. 7-NO2-1,2,3,4-Tetrahydroisoquino-2-yl purine riboside was identified as the analogue with the nitro group in the best orientation at the NBMPR binding site of ENT1. In the present study, further conformational constraining was introduced by synthesizing 5prime-O,8-cyclo derivatives. The flow cytometrically determined binding affinities indicated that the...

2008-01-01

219

Carbohydrates/nucleosides/RNA-DNA-ligand interactions

Biomagnetic separation of Salmonella Typhimurium with high affine and specific ligand peptides isolated by phage display technique

Carbohydrate and nucleotide structural determination using modern spectroscopic techniques is dependent on our ability to label oligonucleotides and oligosaccharides with stable isotopes. Uniform Carbon 13 and Nitrogen 15 labeling of oligonucleotides is important to present-day efforts, which are focused on determining the structure of relatively small oligosaccharides and oligonucleotides, which form the elements of larger structures. Because of the relatively recent interest in three-dimensional structure, the development of techniques used to label them has lagged behind parallel techniques used to label peptides and proteins. Therefore, this group`s discussion focused primarily on problems faced today in obtaining oligonucleotides labeled uniformly with carbon 13 and nitrogen 15.

1994-12-01

220

Apelin, diabetes, and obesity

Analyses of food-borne pathogens are of great importance in order to minimize the health risk for customers. Thus, very sensitive and rapid detection methods are required. Current conventional culture techniques are very time consuming. Modern immunoassays and biochemical analysis also require pre-enrichment steps resulting in a turnaround time of at least 24 h. Biomagnetic separation (BMS) is a promising more rapid method. In this study we describe the isolation of high affine and specific peptides from a phage-peptide library, which combined with BMS allows the detection of Salmonella spp. with a similar sensitivity as that of immunomagnetic separation using antibodies.

2007-04-15

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16

221

British Library Electronic Table of Contents (United Kingdom)

Apelin is a peptide known as the ligand of the G-protein-coupled receptor APJ. Several active apelin forms exist such as apelin-36, apelin-17, apelin-13, and the pyroglutamated form of apelin-13. Apelin and APJ are expressed in the central nervous system, particularly in the hypothalamus and in many peripheral tissues. Apelin has been shown to be involved in the regulation of cardiovascular and fluid homeostasis, food intake, cell proliferation, and angiogenesis. In addition to be an ubiquitous peptide, apelin is also produced and secreted by adipocytes and thus considered as an adipokine. This has opened a new field of investigation establishing a link between apelin and metabolic disorders (obesity, type 2 diabetes, etc.) which is the focus of the present review. Several studies, but not...

2011-01-01

222

A new vanadium Schiff base complex as catalyst for oxidation of alcohols

British Library Electronic Table of Contents (United Kingdom)

The monoanionic bidentate Schiff base, N-(phenolyl)-benzaldimine (HL), has been employed to synthesize a new vanadium(IV) complex of general composition [VO(L)2] (where L = O, N donor of Schiff base). The ligand and complex have been fully characterized by elemental analyses, molar conductance data, FT-IR, 1H- and 13C-NMR, and UV-Vis spectroscopies. Oxidation of alcohols to their corresponding aldehydes and ketones was conducted by this complex catalyst using Oxone as oxidant under biphasic reaction conditions (CH2Cl2/H2O) and tetra-n-butylammonium bromide as phase transfer agent under air at room temperature.

2010-01-01

223

211At-Rh(16-S4-diol) as a starting complex for preparing an astatine-labeled radiopharmaceutical

British Library Electronic Table of Contents (United Kingdom)

A new procedure for preparing an 211At-labeled radiopharmaceutical is suggested. The 211At? anion forms a strong bond with the Rh3+ cation incorporated in the complex with a thiother ligand, 1,5,9,13-tetrathiacyclohexadecane-3,11-diol (16-S4-diol). The reaction conditions are optimized with 131I as astatine analog. The complexes are studied by paper electrophoresis, ion exchange, and thin-layer chromatography. The kinetics of the addition of the 131I? anion to Rh(16-S4-diol) and the dependence of the yield of the forming complex 131I-Rh(16-S4-diol) on the temperature, solution acidity, and reactant concentrations are examined. Taking into account the results obtained, the complex 211At-Rh(16-S4-diol) is prepared by adding astatide (211 At?) to equivalent amounts of RhCl3 and the tetrathioe...

2008-01-01

224

Weakly-bridged dimeric diorganotin(IV) compounds derived from pyruvic acid hydrazone Schiff base ligands: Synthesis, characterization and crystal structures

British Library Electronic Table of Contents (United Kingdom)

We report the synthesis of four diorganotin(IV) compounds of Schiff base pyruvic acid hydrazone derivatives formulated as [R2SnLY]2, where L1 is 2-SC4H3CON2C(CH3)CO2 with Y = CH3CH2CH2CH2OH, R = n-Bu (1); L2 is C6H5CON2C(CH3)CO2 with Y = CH3CH2OH, R = p-F-Bz (2); L3 is 2-HOC6H4CON2C(CH3)CO2 with YH2O, R = p-CN-Bz (3); and L4 is 4-NO2-C6H4CON2C(CH3)CO2 with YCH3CH2OH, R = Bz (4). The structures of all compounds have been established by a combination of single-crystal X-ray diffraction analysis, 1H and 119Sn NMR spectroscopy, IR spectroscopy, and elemental analysis. Studies reveal that four ligands present the same coordination mode with tin center, which all present tridentate ONO donor Schiff bases and coordinate to the tin center in an enolic form. In compounds 1-4, each tin atom is seven...

2011-01-01

225

The interaction of /sup 125/I-insulin with cultured 3T3-L1 adipocytes: quantitative analysis by the hypothetical grain method

Synthesis, structure, and antitumor activity of novel platinum(II) complexes involving asymmetric chiral diamines as carrier ligands

The murine 3T3-L1 fibroblast under appropriate incubation conditions differentiates into an adipocyte phenotype. This 3T3-L1 adipocyte exhibits many of the morphologic, biochemical, and insulin-responsive features of the normal rodent adipocyte. Using quantitative electron microscopic (EM) autoradiography we find that, when /sup 125/I-insulin is incubated with 3T3-L1 adipocytes, the ligand at early times of incubation localizes to the plasma membrane of the cell preferentially to microvilli and coated pits. When the incubation is continued at 37 degrees C, /sup 125/I-insulin is internalized by the cells and preferential binding to the villous surface is lost. With the internalization of the ligand, two intracellular structures become labeled, as determined by the method of hypothetical grain analysis. These include large clear, presumably endocytotic, vesicles and multivesicular bodies. Over the first hour of incubation the labeling of these ...

1983-07-01

226

Synthesis and characterization of ["1"2"5I]-N-(N-benzylpiperidin-4-YL)-4-iodobenz amide, a potential high affinity sigma ligand for imaging breast cancer

New platinum(II) complexes with asymmetrically substituted chiral diamine ligands A{sub 2}PtX{sub 2}, (A{sub 2}=NH{sub 2}CH(CH{sub 3})CH{sub 2}NH(c-C{sub 5}H{sub 9}) (apcpa), NH{sub 2}CH(CH{sub 3})CH{sub 2}NH(c-C{sub 6}H{sub 11}) (apcha); X{sub 2}=2Cl, isopropylidenmalonate (IPM), 1,1'-cyclobutandicarboxylate (CBDCA) have been synthesized and characterized by means of elemental analyses, infrared and NMR spectroscopies, and X-ray crystallography. The crystal structures of (S-apcha)Pt[CBDCA]{center_dot}3H{sub 2}O (orthorhombic, P2{sub 1}2{sub 1}2(No. 18), a=6.926(3), b=15.243(3), c=19.319(4) A, V=2039.5(10) A{sup 3}, Z=4, R=0.072) and (S-apcha)Pt[IPM]{center_dot}2.5H{sub 2}O (monoclinic, P2/c(No. 13), a=9.882(1), b=18.502(1), c=22.056(1) A, V=4032.8(5) A{sup 3}, Z=8, R=0.093) exhibit that the platinum atoms achieve a typical square planar arrangement with two nitrogen atoms in cis position and with the chiral center retained. The spectroscopic data disclose ...

1999-12-01

227

Spectroscopic Studies of Phosphazene Polymers Containing Photoluminescent Metal Complexes

Three regio-isomers of N-(N-benzylpiperidin-4-yl)-4-iodobenzamide, IBP, were prepared and evaluated for their sigma affinities. All three isomers (2, 3, and 4-substituted) showed high affinities for sigma-1 receptors in guinea pig brain membranes (Ki - 1.64 nM, 3.02 nM, 1.70 nM respectively) against ["3H]-(+)-pentazocine, a sigma-1 selective ligand. 2-IBP and 4-IBP showed modest affinities for sigma-2 sites in rat liver (Ki = 29.6 nM. 25.2 nM respectively) against ["3H]DTG in the presence of dextrallorphan to mask sigma-1 sites. The homologous competition binding studies of 4-["1"2"5I]BP in MCF-7 human breast tumor cells showed high affinity dose-dependent binding. Competition binding studies with haloperidol and DTG also showed a high affinity binding (Ki = 4.6 nM, 60 nM respectively), demonstrating the sigma specificity. The saturation binding (Scatchard analysis) of ["3H]DTG with MCF-7 cell membrane preparations gave Kd of 24.54 nM and a Bmax of 2071 fmol/mg ...

1994-08-21

228

British Library Electronic Table of Contents (United Kingdom)

Abstract A series of small phosphazene ligands with pendant 6-phenyl-2,2--bipyridyl moieties, namely L1 [N3P3(OPh)5(OPhbpyPh)], L2 [N3P3(biph)2(OPhbpyPh)2], L3 [N3P3(tBubiph)2(OPhbpyPh)2], L4 [N3P3(biph)2(OPhbpyPh)Cl] and L5 [N3P3(biph)2(OPhbpyPh)(OPh)] [OPhbpyPh = 4-(4-phenoxy)-6-phenyl-2,2--bipyridine, OPh = phenoxy, biph = 2,2--oxybiphenyl and tBubiph = 4,4--di-tert-butyl-2,2--oxybiphenyl], have been used to synthesise the new cyclometallated palladium(II) and platinum(II) complexes [(L1-H)PdCl], [(L1-H)PtCl], [(L1-H)(PdCl)2], [(L3-H)(PdCl)2], [(L4-H)PtCl], [(L5-H)PtCl] and the rhenium(I) complex [L5Re(CO)3Cl]. Single-crystal X-ray diffraction analysis was performed on the free ligand L2 and the palladium complexes [(L1-H)PdCl] and [(L3-H)(PdCl)2]. In both PdII complexes, the metal cent...

2011-01-01

229

Site-specific semisynthetic variant of human hemoglobin

Optical oxygen sensing materials based on a novel dirhenium(I) complex assembled in mesoporous silica

A single round of Edman degradation was employed to remove the NH_2-terminal valine from isolated #alpha# chains of human hemoglobin. Reconstitution of normal #beta# chains with truncated or substituted #alpha# chains was used to form truncated (des-Val"1-#alpha#1) and substituted ([[1-"1"3C]Gly"1]#alpha#1) tetrameric hemoglobin analogs. Structural homology of the analogs with untreated native hemoglobin was established by using several spectroscopic and physical methods. Functional studies indicate that the reconstituted tetrameric protein containing des-Val"1-#alpha# chains has a higher affinity for oxygen, is less influenced by chloride ions or 2,3-biphosphoglycerate, and shows lower cooperativity than native hemoglobin. These results confirm the key functional role of the #alpha#-chain NH_2 terminus in mediating cooperative oxygen binding across the dimer interface. The NH_2-terminal pK/sub 1/2/ value was determined for the ["1"3C]glycine-substituted analog to be 7.46 +/- 0.09 at ...

230

Novel snake venom ligand dendroaspis natriuretic peptide is selective for natriuretic peptide receptor-A in human heart: downregulation of natriuretic peptide receptor-A in heart failure.

A new dirhenium(I) complex fac-[{Re(CO)3(4,7-dinonadecyl-1,10-phenanthro -line)}2 (4,4'-bipyridyl)] (trifluoromethanesulfonate)2 (denoted as D-Re(I) ) is assembled in MCM-41 and SBA-15 type mesoporous silica support. The emission peaks of D-Re(I) in D-Re(I)/MCM-41 and D-Re(I)/SBA-15 are observed at 522 and 517 nm, respectively. Their long excited lifetimes, which are of the order of microseconds, indicate the presence of phosphorescence emission arising from the metal to ligand charge-transfer (MLCT) transition. The luminescence intensities of D-Re(I)/MCM-41 and D-Re(I)/SBA-15 decrease remarkably with increase in the oxygen concentration, meaning that they can be used as optical oxygen sensing materials based on luminescence quenching. The ratios I0/I100 of D-Re(I)/MCM-41 and D-Re(I)/SBA-15 are estimated to be 5.6 and 20.1, respectively. The obtained Stern-Volmer oxygen quenching plots of the mesoporous sensing materials could be fitted well to the two-site Demas ...

2011-04-01

231

New microwave assisted radiolabelling method and rat brain biodistribution study of two new "9"9"mTc-tricarbonyl complexes as potential brain imaging agents

The natriuretic peptides are considered to be cardioprotective; however, their receptors have not been identified in human myocardium using radiolabeled analogs. Dendroaspis natriuretic peptide (DNP) has been recently identified as a new member of this peptide family and is thought to be less susceptible to enzymatic degradation. Therefore, we have developed the novel radiolabeled analog [125I]-DNP and used this to localize high-affinity (K(D)=0.2 nmol/L), saturable, specific binding sites in adult human heart (n=6) and coronary artery (n=8). In competition binding experiments, atrial natriuretic peptide and brain type natriuretic peptide had greater affinity for [125I]-DNP binding sites than C-type natriuretic peptide and the natriuretic peptide receptor (NPR)-C ligand, cANF. This rank order of potency suggested binding of [125I]-DNP was specific to NPR-A. Messenger RNA encoding NPR-A was identified in left ventricle and coronary artery smooth muscle, and ...

2006-06-15

232

In vitro assessment of the agonist properties of the novel 5-HT_1_A receptor ligand, CUMI-101 (MMP), in rat brain tissue

Two new cyclopentadienyl piperidine derivatives, namely ferrocene carboxylic acid 1-ethyl-3-hydroxypiperidinyl ester and ferrocene carboxylic acid 4-hydroxypiperidinyl ester, were synthesized. The ligands were then radiolabelled with "9"9"mTc using two different approaches. The first method consisted of reacting the ligand precursor with Mn(CO)_5Br in pertechnetate "9"9"mTcO_4 - in normal saline and dimethyl formamide (DMF) at 150 "oC for 1 h. The yields were 70% and 90%, respectively. For the second method, the reactions mixtures were placed in a microwave oven for 2 min at 650 watt. The yields were higher than 90% for both "9"9"mTc complexes. Biodistribution studies showed that tricarbonyl[#eta#"5-[carboxy-3-hydroxy(N-ethyl)piperidine]cyclopentadienyl] technetium(I) had the highest brain uptake. The regional distribution in the brain also demonstrated relatively higher uptake of tricarbonyl [#eta#"5-[carboxy-3-hydroxy(N-ethyl) ...

233

Characterization of tris(N-substituted-2-methyl-3-hydroxy-4-pyridinonato)technetium(IV) cations

Introduction: Development of agonist positron emission tomography (PET) radioligands for the 5-HT neurotransmitter system is an important target to enable the understanding of human 5-HT function in vivo. ["1"1C]CUMI-101, proposed as the first 5-HT_1_A receptor agonist PET ligand, has been reported to behave as a potent 5-HT_1_A agonist in a cellular system stably expressing human recombinant 5-HT_1_A receptors. In this study, we investigate the agonist properties of CUMI-101 in rat brain tissue. Methods: ["3"5S]-GTP#gamma#S binding studies were used to determine receptor function in HEK (human embryonic kidney) 293 cells transfected with human recombinant 5-HT_1_A receptors and in rat cortex and rat hippocampal tissue, following administration of CUMI-101 and standard 5-HT1A antagonists (5-HT, 5-CT and 8-OH-DPAT). Results: CUMI-101 behaved as an agonist at human recombinant 5-HT_1_A receptors (pEC_5_0 9.2). However, CUMI-101 did not show agonist activity in either ...

2011-02-01

234

Characterization of tris(N-substituted-2-methyl-3-hydroxy-4-pyridinonato)technetium(IV) cations

A burgeoning interest in technetium coordination chemistry has been spurred by its widespread use in nuclear medicine. Recent focus has been on the design and preparation of new technetium complexes, the lipophilicity, polarity, and overall charge of which can be readily altered by simple substitutions in the molecular framework of the ligand in order to optimize the biodistribution and target specific organs. Examples are cationic (Cardiolite) and neutral (Ceretec) technetium complexes, used as myocardial and brain imaging agents, respectively. The authors have been pursuing a continuing study of tris(3-hydroxy-4-pyridinonato)gallium and -indium complexes that are water soluble, are hydrolytically stable, and are of varying lipophilicity and neutral charge. Studies of in vivo in rabbits and mice have revealed that several of these cationic complexes may be useful as morphologic kidney imaging agents, with [{sup 99m}Tc(pap){sub 3}]{sup +} showing elevated levels in ...

1994-11-23

235

Acid-base behavior of the ground and excited states of platinum(II) complexes of quinoxaline-2,3-dithiolate

A burgeoning interest in technetium coordination chemistry has been spurred by its widespread use in nuclear medicine. Recent focus has been on the design and preparation of new technetium complexes, the lipophilicity, polarity, and overall charge of which can be readily altered by simple substitutions in the molecular framework of the ligand in order to optimize the biodistribution and target specific organs. Examples are cationic (Cardiolite) and neutral (Ceretec) technetium complexes, used as myocardial and brain imaging agents, respectively. The authors have been pursuing a continuing study of tris(3-hydroxy-4-pyridinonato)gallium and -indium complexes that are water soluble, are hydrolytically stable, and are of varying lipophilicity and neutral charge. Studies of in vivo in rabbits and mice have revealed that several of these cationic complexes may be useful as morphologic kidney imaging agents, with ["9"9"mTc(pap)_3]"+ showing elevated levels in the kidneys ...

236

Synthesis, characterization, and crystal structure of neutral rhenium(V) complexes with S-substituted N{sub 2}S{sub 2} ligands

The acid-base behavior of the ground and excited states of Pt(qdt){sub 2}{sup 2{minus}} and Pt(phen)(qdt), where qdt=quinoxaline-2,3-dithiolate and phen = 1,10-phenanthroline, has been studied. The pH-dependent changes in the charge-transfer absorption and emission spectra for both complexes are attributed to protonation of the quinoxalinedithiolate ligand at the imine nitrogen. For Pt(qdt){sub 2}{sup 2{minus}}, single protonation leads to a large red shift (2582 cm{sup {minus}1}) of the low-energy charge-transfer-to-dithiolate absorption band and the emergence of a new red-shifted emission feature at 728 nm. In solutions of pH below 6, a second protonation takes place at the other qdt ligand, yielding Pt-(Hqdt){sub 2}. This neutral complex has been isolated and characterized by {sup 1}H NMR spectroscopy and elemental analyses. The ground-state basicity constants of the two protonation steps have been determined from spectrophotometric ...

1995-06-21

237

Water-soluble cis-[(NHC)PdBr2(TPPTS)] catalysts and their applications in Suzuki-Miyaura coupling of aryl chlorides

Rhenium is technetium`s third row congener and exhibits many of the chemical properties that technetium displays. Theoretically, a Re-PhAT complex will be isostructural with the {sup 99m}Tc PhAT complexes that have been prepared for use as brain imaging agents. A series of neutral rhenium(V) oxo complexes was synthesized by the reaction of ReOBr{sub 4}{sup {minus}} with diamino-thiol-thioether ligands of the type (RSC(CH{sub 3}){sub 2})CH{sub 2}NH(o-C{sub 6}H{sub 4})NHCH{sub 2}C(CH{sub 3}){sub 2}SH. The complexes were characterized by IR, UV/visible, and {sup 1}H and {sup 13}C NMR spectroscopy and by fast-atom-bombardment mass spectroscopy. The single-crystal X-ray structure determination on two of the complexes, where R = CH{sub 2}CH{double_bond}CH{sub 2} and CH{sub 2}CH{sub 2}-CH{sub 3}, showed them to consist of a square pyramidal Re{sup V}ON{sub 2}S{sub 2} core. ReO[CH{sub 2}{double_bond}CHCH{sub 2}SC(CH{sub 3}){sub 2}CH{sub 2}N(o-C{sub 6}H{sub 4})NCH{sub ...

1994-11-23

238

British Library Electronic Table of Contents (United Kingdom)

New palladium(II) complexes (2), bearing NHC/TPPTS ligands, (NHC=benzimidazol-2-ylidene; TPPTS=triphenylphosphine-3,3',3''-trisulfonic acid trisodium salt) have been prepared and characterized by elemental analyses and spectroscopic methods. Their ability to catalyze the Suzuki-Miyaura reaction in neat water has been studied at 100^oC. Very high activities have been observed in the coupling of phenylboronic acid with aryl chlorides in the presence of 1% of the catalyst. We have compared the electronic properties of cis-[PdBr2(NHC)(TPPTS)] with the related complexes, [PdX2(NHC)]2 and [trans-PdBr2(NHC)(pdca)] (pdca=pyridine-2,6-dicarboxyic acid) (3) via three different techniques: cyclic voltammetry, thermogravimetric analysis and ^1^3C NMR spectroscopy.

2011-01-01

239

The crystal structure Escherichia coli Spy.

The chemistry of technetium(V) complexes containing tetradentate amine oxime ligands

Escherichia coli spheroplast protein y (EcSpy) is a small periplasmic protein that is homologous with CpxP, an inhibitor of the extracytoplasmic stress response. Stress conditions such as spheroplast formation induce the expression of Spy via the Cpx or the Bae two-component systems in E. coli, though the function of Spy is unknown. Here, we report the crystal structure of EcSpy, which reveals a long kinked hairpin-like structure of four ?-helices that form an antiparallel dimer. The dimer contains a curved oval shape with a highly positively charged concave surface that may function as a ligand binding site. Sequence analysis reveals that Spy is highly conserved over the Enterobacteriaceae family. Notably, three conserved regions that contain identical residues and two LTxxQ motifs are placed at the horizontal end of the dimer structure, stabilizing the overall fold. CpxP also contains the conserved sequence motifs and has a predicted secondary structure similar ...

2010-11-01

240

Technetium-99m dithiocarbamates as potential agents for brain imaging

Technetium-99m was previously shown to form a stable, neutral and lipopholic complex with propylene amine oxime, PnAO. This Tc-99m-PnAO complex was shown to efficiently extracted by normal brain. However, it is not sufficiently retained in the brain to image its cerebral distribution using convertional SPECT (single-photon emission computerized tomography) instrumentation. A number of derivatives of PnAO have been synthesized and their technetium-99m complexes have been biologically evaluated. A number of these have been shown to have high brain uptake without exhibiting the rapid cerebral clearance that was observed with Tc-99m-PnAO. To better understand the chemistry of these potential brain imaging agents, a number of technetium-99 complexes of derivatives of PnAO have been synthesized and characterized. Substituents on the tetradentate amine oxime backbone were varied to probe the effect(s) of these structural changes on the properties of the resultant Tc(V) complexes.

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16

241

Synthesis, crystal structure and spectroscopic studies of copper(II) complex of C-meso-1,5,8,12-tetramethyl-1,4,8,11-tetraazacyclotetradecane

Thallium-201 diethyldithiocarbamate (DDC) behaves like a chemical microsphere and is trapped by spontaneous decomposition in the brain in proportion to regional perfusion. They have shown that the technetium-99m analog, Tc-99m DDC (1), is unsuitable for cerebral perfusion imaging because it does not decompose rapidly enough to be trapped in the brain. With the goal of turning this greater stability of 1 into an advantage, a series of dithiocarbamates with lipophilic or amine groups designed to enhance cerebral uptake and retention was prepared from the following amines by reaction with carbon disulfide and sodium hydroxide: pyrrolidine (2), piperazine (3), 4-benzylpiperazine (4), and 4-(1-piperidino)piperidine (5). These ligands (5 mg) were labelled with Tc-99m in > 95% efficiency (ITLC-SG, saline) by reduction of pertechnetate at room temperature with formamidine sulfinic acid at alkaline pH. In preliminary studies, 4 and 5 show a trend of increasing oil/buffer ...

242

British Library Electronic Table of Contents (United Kingdom)

Copper(II) complex coordinated with cyclam-type macrocyclic tetramine, C-meso-1,5,8,12-tetramethyl-1,4,8,11-tetraazacyclotetradecane (2Cdmc) has been synthesized and characterized by single crystal X-ray crystallographic analysis and UV?Vis absorption spectra. Solved molecular structure of [Cu(2Cdmc)(H2O)]Cl2?2H2O (1) revealed that macrocyclic ligand 2Cdmc was in the most stable trans-III structure, but the C-methyl groups of 2Cdmc adopted energetically unfavorable axial configuration (C-axial). This complex 1 is the second example of complex of cyclam-type tetramine with only axially oriented C-methyl groups. This complex adopted five-coordinated square-pyramidal geometry with one water molecule occupying one of the two apical sites. Network of hydrogen bonds involving counter anions (Cl?...

2011-01-01

243

Synthesis of (diamine)platinum(II) and (diamine)platinum(IV) complexes of isopropylidenmalonate ligand and their interaction with guanosine-5'-monophosphate

Study of the electron paramagnetic resonance spectra of Zn(antipyrine)_2(NO_3)_2:VO"2"+

A series of (diamine)isopropylidenmalonatoplatinum(II) complexes and the oxidation products, (diamine)Pt(OOC){sub 2}C=C(CH{sub 3}){sub 2}(X){sub 2}, (diamine=ethylenediamine(en), 1,2-diaminopropan(dap), N-methylethylenediamine(men); X=OH, OCOCH{sub 3}, OCOCF{sub 3}), have been prepared, and their interaction with guanosine-5'-monophosphate (5'-GMP) have been examined by means of {sup 1}H NMR spectroscopy. The present platinum(II) complexes have shown to interact with 5'-GMP through N7 coordination in two consecutive steps in a similar way as with cisplatin, but no interaction between the present platinum(IV) complexes and 5'-GMP was observed. However, in the presence of ascorbic acid, the platinum(IV) complexes have been found to interest with 5'-GMP with the reation rate depending on their reduction rate.

1998-10-01

244

Studies of the involvement of metal ions with several medicinal agents

In this work, a full ligand-field energy matrix (10x10) diagonalization treatment for 3d"1 ions in tetragonal symmetry is developed on the basis of the two-s.o.-coupling-parameter model. Spin Hamiltonian parameters (g factors g_|_|, g_p_e_r_p_e_n_d_i_c_u_l_a_r and hyperfine structure constants A_|_|, A_p_e_r_p_e_n_d_i_c_u_l_a_r) of the tetragonal V"4"+ center in Zn(antipyrine)_2(NO_3)_2 are calculated from the complete energy matrix diagonalization method and the perturbation theory method. The calculated results from both methods are not only close to each other but also in good agreement with the experimental values. Furthermore, the compressed defect structure of V"4"+ center is discussed.

2010-08-01

245

Preparation and biodistribution of technetium-99m-labeled 1-(2-nitroimidazole-1-yl)-propanhydroxyiminoamide (N2IPA) as a tumor hypoxia marker

NMR and CD studies indicate that Mg/sup 2 +/ and Ca/sup 2 +/ are able to change the conformation of tetracycline in DMSO solution. This may affect the in vivo effect of tetracycline. Using /sup 23/Na NMR, the formation constant of NaLAS (LAS represents the anion of lasalocid A) was found to be 80 M/sup -1/ which is much smaller than that in less polar solvents. Spin-lattice relaxation measurements were made to study the binding sites of Gd/sup 3 +/ on Las in ChCl/sub 3/-DMF mixed solvent system. No intermediate conformation (between cyclic and open-chain) was found. LAS was found to be a good second-sphere ligand to inert transition-metal amines. NMR studies suggest that LAS is in cyclic conformation when bound to these metal amines. A new method for the synthesis of spin-labeled anticancer Pt(II) complexes was developed. It is very simple and gives high yield of pure spin-labeled Pt(II) complexes.

1985-01-01

246

Preclinical evidence for the benefits of penile rehabilitation therapy following nerve-sparing radical prostatectomy.

A new hydroxyiminoamide ligand, 1-(2-nitroimidazole-1-yl)-propanhydroxyiminoamide (N2IPA) was synthesized. The biodistribution of {sup 99m}Tc-N2IPA in mice bearing S180 tumor demonstrated that the complex showed a selective accumulation in tumor and slow clearance from it. The tumor-to-tissue uptake ratios increased with time. At 4 hours after injection, the uptake ratios of tumor to muscle, blood, liver, heart, and lung reached 8.4, 1.5, 0.6, 2.9, and 2.3, respectively. Moreover, the tumor-to-liver uptake ratio steadily increased to 0.9 at 8 hours and 2.3 at 24 hours. The complex showed little uptake and quick clearance in blood, lung and other organs. Compared with other proposed hypoxia-imaging agents, this novel agent has advantages of higher tumor-to-muscle and tumor-to-blood uptake ratios and easier synthesis.

2004-02-01

247

Polyphenol rich botanicals used as food supplements interfere with EphA2-ephrinA1 system

Erectile dysfunction following radical prostatectomy remains a frequent problem despite the development of nerve-sparing techniques. This erectile dysfunction is believed to be neurogenic, enhanced by hypoxia-induced structural changes which result in additional veno-occlusive dysfunction. Recently, daily use of intracavernous vasoactive substances and oral use of PDE5-inhibitors have been clinically studied for treatment of postprostatectomy erectile dysfunction. Since these studies showed benefits of "penile rehabilitation therapy," these effects have been studied in a preclinical setting. We reviewed experimental literature on erectile tissue preserving and neuroregenerative treatment strategies, and found that preservation of the erectile tissue by the use of intracavernous nitric oxide donors or vasoactive substances, oral PDE5-inhibitors, and hyperbaric oxygen therapy improved erectile function by antifibrotic effects and preservation of smooth muscle. Furthermore, ...

2008-01-01

248

British Library Electronic Table of Contents (United Kingdom)

The Eph tyrosine kinase receptors and their ephrin ligands play a central role in several human cancers and their deregulated expression or function promotes tumorigenesis, inducing aggressive tumor phenotypes. Green tea extracts (GTE) have been recently found to inhibit Eph-kinase phosphorylation. In order to evaluate the potential contribution of edible and medicinal plants on EphA2-ephrinA1 modulation, 133 commercially available plant extracts used as food supplements, essential and fixed oils were screened with an ELISA-based binding assay. Nine plant extracts, rich of polyphenols, reversibly inhibited binding in a dose-dependent manner (IC"5"0 0.83-24@mg/ml). Functional studies on PC3 prostate adenocarcinoma cells revealed that active extracts antagonized ephrinA1-Fc-induced EphA2-pho...

2011-01-01

249

Pharmacodynamics of a novel designer natriuretic peptide, CD-NP, in a first-in-human clinical trial in healthy subjects.

Palladium(II) and platinum(II) saccharinate complexes containing pyridine and 3-acetylpyridine: Synthesis, crystal structures, fluorescence and thermal properties

CD-NP is a novel chimeric natriuretic peptide (NP) consisting of the 22-amino-acid (AA) human C-type natriuretic peptide (CNP), a venodilating peptide with limited renal actions and minimal effects on blood pressure, and the 15-AA C-terminus of Dendroaspis NP (DNP). The rationale for the design of CD-NP was to enhance the renal actions of CNP, the ligand for natriuretic peptide receptor-B, but without inducing excessive hypotension. Here we report the first-in-human studies for CD-NP, which represent the first successful clinical testing of a chimeric NP demonstrating in normal human volunteers that CD-NP possesses cyclic guanosine monophosphate-activating, natriuretic, and aldosterone-suppressing properties without inducing excessive hypotension, laying the foundation for additional studies on this first-in-class new cardiovascular therapeutic in human heart failure, which are now underway worldwide. PMID:19395584

2009-04-24

250

British Library Electronic Table of Contents (United Kingdom)

New palladium(II) and platinum(II) complexes of saccharinate (sac), trans-[Pd(py)"2(sac)"2] (1), cis-[Pt(py)"2(sac)"2] (2), trans-[Pd(3-acpy)"2(sac)"2] (3) and cis-[Pt(3-acpy)"2(sac)"2] (4) (py=pyridine and 3-acpy=3-acetylpyridine) have been synthesized. Elemental analysis, UV-Vis, IR, NMR and TG/DTA characterizations have been carried out. The structures of 1-4 were determined by X-ray diffraction. The palladium(II) and platinum(II) ions are coordinated by two N-bonded sac ligands, and two nitrogen atoms of py or 3-acpy, forming a distorted square-planar geometry. The palladium(II) complexes (1 and 3) are trans isomers, while the platinum(II) complexes (2 and 4) are cis isomers. The mononuclear species in the solid state are connected by weak intermolecular C-H...O hydrogen bonds, C-H...@...

2011-01-01

251

Online immunoaffinity LC/MS/MS. A general method to increase sensitivity and specificity: How do you do it and what do you need?

Novel non-discoid chiral copper(II)-salen type [N2O2] donor Schiff base complexes with a cyclohexane diamine spacer: synthesis, electrochemistry, columnar mesomorphism and DFT study

There is an increased emphasis on hyphenated techniques such as immunoaffinity LC/MS/MS (IA-LC/MS/MS) or IA-LC/MRM. These techniques offer competitive advantages with respect to sensitivity and selectivity over traditional LC/MS and are complementary to ligand binding assays (LBA) or ELISA's. However, these techniques are not entirely straightforward and there are several tips and tricks to routine sample analysis. We describe here our methods and procedures for how to perform online IA-LC/MS/MS including a detailed protocol for the preparation of antibody (Ab) enrichment columns. We have included sample trapping and Ab methods. Furthermore, we highlight tips, tricks, minimal and optimal approaches. This technology has been shown to be viable for several applications, species and fluids from small molecules to proteins and biomarkers to PK assays. PMID:21872661

2011-08-22

252

British Library Electronic Table of Contents (United Kingdom)

A series of new non-discoid chiral copper(ii)-salen type complexes, [Cu((4-CnH2n+1O)2salen)], n = 14, 16, 18 and salen = N,N'-cyclohexane bis (salicylideneiminato), containing 4-substituted alkoxy tails in the side aromatic rings and a cyclohexane spacer, have been prepared and their mesogenic properties investigated. The compounds were characterised by Fourier transform infra-red spectroscopy, 1H and 13C nuclear magnetic resonance spectroscopy, UV-vis spectroscopy and fast atom bombardment mass spectrometry. Mesomorphic properties of these compounds were studied by polarising optical microscopy, differential scanning calorimetry and X-ray diffraction (XRD). The ligands are non-mesogenic but the complexes exhibited enantiotropic rectangular columnar mesophases (Colr) with extended temperat...

2011-01-01

253

New Tc-99m brain imaging agents

New Tc-99m brain imaging agents

In developing new Tc-99m brain perfusion imaging agents for SPECT, a series of BAT (bis-aminoethanethiol) derivatives was prepared. These N/sub 2/S/sub 2/ ligands formed stable and neutral complexes with reduced Tc-99m, either by Sn(II)-PPi or sodium borohydride reduction. The purity of the Tc-99m complexes was >95% (HPLC reverse-phase column, acetonitrile: pH 7.0 buffer, 85:15). The biodistribution in rats was evaluated using I-125 iodoantipyrine (IAP), a free diffusible tracer, as the internal reference. Compounds with a free hydroxyl group (I and IV) showed lower brain uptake, inspite of high P.C.; this may be related to in vivo instability of the complexes. High initial brain uptake was observed for three compounds (II, III and V), however, only compound V (P.C.=384) showed significant brain retention. Planar imaging with compound V in a monkey demonstrated that the compound localized in brain and the retention time was T/sub 1/2/=35 min. Compounds of this ...

1984-01-01

254

New Insights into the Design of Inhibitors of Human S-Adenosylmethionine Decarboxylase: Studies of Adenine C[superscript 8] Substitution in Structural Analogues of S-Adenosylmethionine

1984-06-05

255

Molybdenum complexes of biochemical interest. New coordination complexes of oxomolybdenum(V) with the tridentate ONO donor Schiff bases derived from salicylaldehydes and ethanolamine

S-Adenosylmethionine decarboxylase (AdoMetDC) is a critical enzyme in the polyamine biosynthetic pathway and depends on a pyruvoyl group for the decarboxylation process. The crystal structures of the enzyme with various inhibitors at the active site have shown that the adenine base of the ligands adopts an unusual syn conformation when bound to the enzyme. To determine whether compounds that favor the syn conformation in solution would be more potent AdoMetDC inhibitors, several series of AdoMet substrate analogues with a variety of substituents at the 8-position of adenine were synthesized and analyzed for their ability to inhibit hAdoMetDC. The biochemical analysis indicated that an 8-methyl substituent resulted in more potent inhibitors, yet most other 8-substitutions provided no benefit over the parent compound. To understand these results, we used computational modeling and X-ray crystallography to study C{sup 8}-substituted adenine analogues bound in the ...

2009-04-02

256

Molybdenum complexes of biochemical interest. New coordination complexes of oxomolybdenum(V) with the tridentate ONO donor Schiff bases derived from salicylaldehydes and ethanolamine

New oxomolybdenum(V) complexes MoOClL (where LH/sub 2/ = Schiff base) derived from ethanolamine and salicylaldehyde, 5-chlorosalicylaldehyde, 5-bromosalicylaldehyde, 5-nitrosalicylaldehyde, 3-ethoxysalicylaldehyde and 2-hydroxy-1-naphthaldehyde have been synthesized and characterised by elemental analyses, conductance, molecular weight, I.R. and electronic spectra and magnetic measurements. The Schiff bases behave as dibasic tridentate ONO donor ligands. The complexes are non-electrolytes and dimers. The complexes exhibit subnormal magnetic moments and are involved in antiferromagnetic exchange with S = 0 ground state. The complexes exhibit electronic spectral bands at ca. 13000 and ca. 17000 cm/sup -1/ due to the transitions dsub(xy)- > dsub(xz,yz) (/sup 2/B/sub 2/- > /sup 2/E) and dsub(xy)- > dsub(x2-y2) (/sup 2/B/sub 2/- > /sup 2/B/sub 1/), respectively. The ..nu..(Mo = O) frequency of the complexes is observed in the 900-970 cm/sup -1/ region. On ...

1985-02-01

257

Ligand carrier protein genes expressed in larval chemosensory organs of Bombyx mori

New oxomolybdenum(V) complexes MoOClL (where LH_2 = Schiff base) derived from ethanolamine and salicylaldehyde, 5-chlorosalicylaldehyde, 5-bromosalicylaldehyde, 5-nitrosalicylaldehyde, 3-ethoxysalicylaldehyde and 2-hydroxy-1-naphthaldehyde have been synthesized and characterised by elemental analyses, conductance, molecular weight, i.r. and electronic spectra and magnetic measurements. The Schiff bases behave as dibasic tridentate ONO donor ligands. The complexes are non-electrolytes and dimers. The complexes exhibit subnormal magnetic moments and are involved in antiferromagnetic exchange with S = 0 ground state. The complexes exhibit electronic spectral bands at ca. 13000 and ca. 17000 cm"-"1 due to the transitions dsub(xy)->dsub(xz,yz) ("2B_2->"2E) and dsub(xy)->dsub(x2-y2) ("2B_2->"2B_1), respectively. The #nu#(Mo=O) frequency of the complexes is observed in the 900-970 cm"-"1 region. On the basis of the magnetic susceptibility, i.r. and molecular ...

1985-01-01

258

British Library Electronic Table of Contents (United Kingdom)

Expressed sequence tags (ESTs) of the maxillary galea of the silkworm were analyzed to identify proteins involved in food selection systems. From the 1251 redundant genes of the ESTs, we identified 7 odorant-binding protein-like genes (bmObpL), 6 takeout-like genes (bmToL), and 6 chemosensory protein genes (bmCsp). Quantitative RT-PCR analysis indicated that bmObpL1, bmObpL2, bmObpL3, bmObpL5, bmToL1, bmToL3, and bmorCsp15 were predominantly expressed in the larval oral appendages, such as the maxilla, labrum, labium and antenna. Immunocytochemical analysis indicated that the proteins of bmObpL1, bmObpL3, and bmToL1 were localized in the gustatory chemosensilla on the maxillary galea and olfactory sensilla in the antenna. The proteins encoded by bmObpL1 and bmObpL3 were detected in the gus...

2011-01-01

259

Inhibitory effect of minocycline on osteoclastogenesis in mouse bone marrow cells

British Library Electronic Table of Contents (United Kingdom)

Objective: To study the effects of minocycline hydrochloride (MINO) on the formation of tartrate-resistant acid phosphatase (TRAP) staining-positive multinucleated osteoclast-like cells in mouse bone marrow cells (BMCs) treated with 1@a,25(OH)"2D"3 or soluble receptor activator of nuclear factor-@kB ligand (s-RANKL). Materials and methods: Mouse BMCs were cultured in alpha-modified minimum essential medium containing foetal calf serum (10%) and tetracyclines (2.5, 5 and 10@mM), such as MINO, tetracycline hydrochloride (TC), oxytetracycline hydrochloride (OXT) or doxycycline (DOXY) in the presence of 1@a,25(OH)"2D"3 (10nM) or s-RANKL (20ng/ml) for 7 days, and the number of TRAP staining-positive osteoclast-like cells was counted. In RNA isolated from BMCs treated with 1@a,25(OH)"2D"3 or s-R...

2011-01-01

260

Functionalized multi-walled carbon nanotubes as affinity ligands

Electron spin resonance study of the equilibrium between tetrahalogeno- and pentahalogeno-nitridotechnetate (VI) ions in solution

Functionalization of carbon nanotubes is very challenging for their applications. The paper here describes a new method to functionalize multi-walled carbon nanotubes (MWCNTs) as specific affinity adsorbents. MWCNTs were acid purified and pretreated with (3-aminopropyl)-triethoxysilane (APTES) in order to introduce abundant amino groups on the surface of MWCNTs. After the conversion of amino groups to carboxyl groups by succinic acid anhydride, MWCNTs were attached to protein A or aminodextran using 1-ethyl-3,3' (dimethylamion)-propylcarbodiimide as a biofunctional crosslinker. The incorporation of aminodextran as a spacer arm noticeably increased the binding capacity of the APTES-modified MWCNTs for protein A. The application of affinity MWCNTs for purification of immunoglobulin G was then evaluated. The affinity of MWCNTs with AMD spacer exhibited a high adsorption capacity of {approx}361 {mu}g IgG/mg MWCNT (wet basis). About 75% of bound IgG was eluted from affinity MWCNTs ...

2007-03-21

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16

261

Dodecanuclear rhenium cluster complexes with an interstitial carbon atom: Synthesis, structures and properties of two new compounds K6[Re12CS17(OH)6]?4H2O and Na12Re12CS17(SO3)6?48.5H2O

The e.s.r. spectra of (AsPh/sub 4/)(TcNCl/sub 4/), Cs/sub 2/(TcNCl/sub 5/), (AsPh/sub 4/)(TcNBr/sub 4/), and Cs/sub 2/(TcNBr/sub 5/) have been studied in non-aqueous and concentrated aqueous acid solutions. None of the spectra shows evidence for the co-ordination of a fifth halide ligand in the trans position, even under circumstances such as a 2 000-fold excess of halide ion, which would be expected to favour the formation of the pentahalogenonitridotechnetate ion. The predominant species in solution is the tetrahalogenonitridotechnetate ion, where the trans position may be vacant or occupied by a solvent molecule in the case of the non-aqeuous solvents and by a water molecule in the case of HCl and HBr solutions. This conclusion may be contrasted with the behaviour of a number of tetra- and penta-halogeno-oxometal complexes, where the equilibrium (MOX/sub 4/)sup(n-) + X/sup -/< - - > (MOX/sub 5/)sup(n + 1)/sup -/ is clearly established.

1987-07-01

262

British Library Electronic Table of Contents (United Kingdom)

The dodecanuclear rhenium anionic complex with terminal hydroxo ligands [Re12CS17(OH)6]6? was obtained by the reaction of K6[Re12CS17(CN)6]?20H2O with molten KOH at 300 ?C. The cluster complex was crystallized as a potassium salt from aqueous solution. The reaction between K6[Re12CS17(OH)6]?4H2O and Na2S2O4 in water under reflux results in the formation of the complex Na12[Re12CS17(SO3)6]?48.5H2O. Both new compounds were characterized by single-crystal X-ray diffraction, elemental analyses and IR spectroscopy. The electronic structure of [Re12CS17(OH)6]6? was also elucidated by DFT calculation

2010-01-01

263

Direct photoaffinity labeling by nucleotides of the apparent catalytic site on the heavy chains of smooth muscle and Acanthamoeba myosins

Crystalline O,O'-di-sec-butyl and O,O'-diethyl dithiophosphate platinum(II) complexes: Synthesis, 13C and 31P CP/MAS NMR, single crystal X-ray diffraction studies and thermal behaviour

The heavy chains of Acanthamoeba myosins, IA, IB and II, turkey gizzard myosin, and rabbit skeletal muscle myosin subfragment-1 were specifically labeled by radioactive ATP, ADP, and UTP, each of which is a substrate or product of myosin ATPase activity, when irradiated with uv light at 0"0C. With UTP, as much as 0.45 mol/mol of Acanthamoeba myosin IA heavy chain and 1 mol/mol of turkey gizzard myosin heavy chain was incorporated. Evidence that the ligands were associated with the catalytic site included the observations that reaction occurred only with nucleotides that are substrates or products of the ATPase activity; that the reaction was blocked by pyrophosphate which is an inhibitor of the ATPase activity; that ATP was bound as ADP; and that label was probably restricted to a single peptide following limited subtilisin proteolysis of labeled Acanthamoeba myosin IA heavy chain and extensive cleavage with CNBr and trypsin of labeled turkey gizzard myosin heavy ...

264

British Library Electronic Table of Contents (United Kingdom)

Crystalline bis(O,O'-di-sec-butyldithiophosphato)platinum(II) was prepared and studied by means of 13C, 31P CP/MAS NMR spectroscopy and single-crystal X-ray diffraction. The unit cell of the platinum(II) compound is comprised of one centrosymmetric mononuclear molecule [Pt{S2P(O-sec-C4H9)2}2], in which the dithiophosphate groups display structural equivalence in both 31P NMR and XRD data. A pair of the dithiophosphate ligands exhibit the same S,S'-bidentate chelating structural function and form two planar four-membered chelate rings, [PtS2P], in this molecule. The planar configuration of the [PtS4] chromophore in structure 1 is governed by the dsp2-hybrid state of platinum(II). The structural states of the dithiophosphate groups in two different samples of complex 1 (one crystallised from...

2011-01-01

265

Chemistry and morphology of coal liquefaction. Quarterly report, January 1-March 30, 1981

Chemical contaminants on DOE lands and selection of contaminant mixtures for subsurface science research

In the course of observing by means of Auger spectroscopy graphite gasification reactions catalyzed by metals, it has been found that in the presence of hydrogen, nickel appears to diffuse from the surface into the bulk of the graphite. When potassium is deposited on graphite, it is volatilized above 400/sup 0/C. Surprisingly the production of methane and carbon dioxide from the reaction of graphite and steam was catalyzed by potassium at as low a temperature as 250/sup 0/C. It has been shown that literature on the alkylation of benzene with synthesis gas is erroneous and that the products reported are due to Lewis acid catalyzed cracking of benzene. A novel cobalt mediated, reversible cleavage of a vinyl-hydrogen bond has been discovered. All products from the thermal decomposition of tetralin have been identified. The stereochemistry of cis-1, 2 dihydrotetralin was determined. In the utilization of the water gas shift reaction as a reducing agent for model coal compounds it has been ...

1981-03-01

266

Characterisation of polynuclear aromatic sulfur-heterocycles in a coal extract by GC/MS

This report identifies individual contaminants and contaminant mixtures that have been measured in the ground at 91 waste sites at 18 US Department of Energy (DOE) facilities within the weapons complex. The inventory of chemicals and mixtures was used to identify generic chemical mixtures to be used by DOE's Subsurface Science Program in basic research on the subsurface geochemical and microbiological behavior of mixed contaminants (DOE 1990a and b). The generic mixtures contain specific radionuclides, metals, organic ligands, organic solvents, fuel hydrocarbons, and polychlorinated biphenyls (PCBs) in various binary and ternary combinations. The mixtures are representative of in-ground contaminant associations at DOE facilities that are likely to exhibit complex geochemical behavior as a result of intercontaminant reactions and/or microbiologic activity stimulated by organic substances. Use of the generic mixtures will focus research on important mixed ...

1992-04-01

267

Biophysical analysis of DNA modified by 1,2-diaminocyclohexane platinum(II) complexes

Polynuclear aromatic sulphur heterocycles (PASHs) were isolated from a coal extract by two-step separation method using silica gel column chromatography and ligand exchanges thin layer chromatography (PdCl{sub 2}/SiO{sub 2}). The subfraction was examined by capillary column gas chromatography with flame ionization detector and flame photometric detector and gas chromatography - mass spectrometry. Identification was accomplished by comparison of chromatographic retention indices and mass spectra of compounds with those reported in the literature. It was found that the principal structures of the sulphur-containing fraction of Guiding coal extract have 3-4 aromatic rings. Dibenzothiophene, C{sub 1} - C{sub 3} alkylated dibenzothiophenes, benzonaphthothiophene and its alkylated derivatives were the main compounds. Only a few other polynuclear sulfur heterocycles were detected. No benzothiophene and its derivatives were presented. 8 refs., 2 figs., 3 tabs.

1994-06-01

268

Assembly of Linear Nano-Chains from Iron Oxide Nanospheres with Asymmetric Surface Chemistry

Modification of DNA and double-stranded deoxyoligonucleotides with antitumor 1,2-diamino-cyclohexanedinitroplatinum(II) (Pt-dach) complexes was investigated with the aid of physico-chemical methods and chemical probes of nucleic acid conformation. The three Pt-dach complexes were used which differed in isomeric forms of the dach non-leaving ligand-Pt(1R,2R-dach), Pt(1S,2S-dach) and Pt(1R,2S-dach) complexes. The latter complex has lower antitumor activity than the other two Pt-dach complexes. Pt(1R,2S-dach) complex exhibits the slowest kinetics of its binding to DNA and of the conversion of monofunctional binding to bifunctional lesions. The anomalously slow electrophoretic mobility of multimers of the platinated and ligated oligomers suggests that bifunctional binding of Pt-dach complexes to a d(GG) site within double-stranded oligonucleotides induces bending of the oligomer. It is proposed that different effects of the Pt-dach complexes on DNA observed in this ...

1992-01-25

269

Antiferromagnetic exchange in a bis(imido) uranium (V) dimeric complex

Besides the multifunctionality, another equally important aspect of nanoparticles is their engineerability to control the geometrical and chemical properties during fabrication. In this work, we exploited this aspect to define asymmetric surface chemistry of an iron oxide nanosphere by controlling the topology of ligand expression on its surface resulting in a particle with two faces, one displaying only amines and the other only thiols. Specifically, amine-functionalized iron oxide nanospheres were attached on a solid support via a crosslinker containing a disulfide bridge. Liberation of the nanosphere using thiolytic cleavage created thiols on the portion of the particle's surface that interacted with the solid support. Employing a solid-phase strategy and a step-by-step addition of particles, the two unique faces on the same nanosphere served as fittings to assemble them into linear nano-chains. Assembly of chains with various lengths and aspect ratios was ...

2011-01-06

270

Analysis of the quantitative structure activity relationship of technetium-99m-labeled diaminedithiol (DADT) and propyleneamineoxime (PAO) brain blood flow analogues

Magnetic coupling between two or more metal centers is an important facet of d- and f-block transition metal chemistry due to its implications in chemical bonding. With respect to actinide metals, magnetic coupling between polymetallic actinide centers is less well-known. Of the few documented examples, only one bimetallic uranium(V) complex, [(MeC{sub 5}H{sub 4}){sub 2}U]{sub 2}[{mu}-1,4-N{sub 2}C{sub 6}H{sub 4}] (1), has unequivocally demonstrated antiferromagnetic coupling. This complex employs a {pi}-conjugated 1,4-phenylenedimide ligand system which bridges the two f{sup 1}-metal centers and enables antiferromagentic coupling between unpaired f-e1ectrons residing in a {pi}-symmetry orbital. In this communication, we report the synthesis of a dimeric bis(imido) uranium(V) iodide complex and demonstrate with magnetic susceptibility measurements and density functional theory (DFT) calculations that the f{sup 1}-uranium centers display antiferromagnetic coupling ...

2008-01-01

271

An electron spin resonance study of the equilibrium between tetrahalogeno- and pentahalogeno-nitridotechnetate (VI) ions in solution

In the search for new brain imaging agents for use with single photon emission computed tomography (SPECT), quantitative structure activity relationship (QSAR) analysis of the correlations between initial brain uptake and physicochemical parameters like lipophilicity, log P, molecular weight, log MW and log U/D (undissociated/dissociated), of the {sup 99m}Tc-DADT (diaminedithiol) complexes and {sup 99m}Tc-PAO (propyleneaminoxime) complexes have been analyzed. High correlations are found for both the {sup 99m}Tc-DADT complexes (r = 0.94) and for the {sup 99m}Tc-PAO complexes (r = 0.83) which are significant at 99.9 and 99.5 percentile level, respectively. These results will help the further design of better ligands for {sup 99m}Tc in brain imaging. (author).

1991-01-01

272

A non-linear approach to the structure-mobility relationship in protein main chains

The e.s.r. spectra of [AsPh_4][TcNCl_4], Cs_2[TcNCl_5], [AsPh_4][TcNBr_4], and Cs_2[TcNBr_5] have been studied in non-aqueous and concentrated aqueous acid solutions. None of the spectra shows evidence for the co-ordination of a fifth halide ligand in the trans position, even under circumstances such as a 2 000-fold excess of halide ion, which would be expected to favour the formation of the pentahalogenonitridotechnetate ion. The predominant species in solution is the tetrahalogenonitridotechnetate ion, where the trans position may be vacant or occupied by a solvent molecule in the case of the non-aqeuous solvents and by a water molecule in the case of HCl and HBr solutions. This conclusion may be contrasted with the behaviour of a number of tetra- and penta-halogeno-oxometal complexes, where the equilibrium [MOX_4]sup(n-) + X"-< - - > [MOX_5]sup(n + 1)"- is clearly established. (author).

273

A non-linear approach to the structure-mobility relationship in protein main chains

A correlation investigation was carried out on the series of atomic coordinates (MPV) and temperature factor (T {sub f}), respectively for human hemoglobin and HIV-1 protease protein main chains. The MPV series revealed resemblances to the corresponding T {sub f} series. Each minor or major peak in a series had a corresponding peak in the related series. This brings a qualitative evidence for the connection of the two parameters. The series were further subjected to spectral and detrended fluctuation analysis which all revealed long-range correlation properties. This combined analysis revealed that the data were controlled both by the correlation of stationary fluctuation and trends or non-stationary contribution to correlation. The correlation of all MPV series was found to be much less sensitive to ligand binding than the corresponding T {sub f} series. Thus the long-range correlation properties of the protein main chain structure and mobility revealed two ...

2007-05-15

274

"2"1"1At-Rh(16-S4-diol) - initial complex of radiopharmaceuticals labelled with astatine

A correlation investigation was carried out on the series of atomic coordinates (MPV) and temperature factor (T _f), respectively for human hemoglobin and HIV-1 protease protein main chains. The MPV series revealed resemblances to the corresponding T _f series. Each minor or major peak in a series had a corresponding peak in the related series. This brings a qualitative evidence for the connection of the two parameters. The series were further subjected to spectral and detrended fluctuation analysis which all revealed long-range correlation properties. This combined analysis revealed that the data were controlled both by the correlation of stationary fluctuation and trends or non-stationary contribution to correlation. The correlation of all MPV series was found to be much less sensitive to ligand binding than the corresponding T _f series. Thus the long-range correlation properties of the protein main chain structure and mobility revealed two complementary ...

2007-05-01

275

Structures and luminescent properties of new uranyl-based hybrid materials

Paper describes a new procedure to synthesize a pharmaceutical containing "2"1"1At. "2"1"1At"- anion was found to bind strongly with Rh"3"+ cation complexing with a thio-ether ligand - 1,5,9,13-tetratiacyclohexadecane-3,11-diol (16-S4-diol). One made use of "1"3"1I isotope to seek for the optimal conditions of the reaction. The derived complexes were studied by means of the paper electrophoresis, the ion exchange, the surface chromatography. One studied the kinetics of "1"3"1I"- anion binding with Rh(16-S4-diol), the dependence of the yield of "1"3"1I-Rh(16-S4-diol) forming complex on the temperature. the acidity of the reaction mixture and the concentration of the reagents. On the basis of the determined conditions of the synthesis one prepared "2"1"1At-Rh(16-S4-diol) complex by more astatide ("2"1"1At"-) to the equivalent amounts of RhCl_3 and tetra-thio-ether (16-S4-diol). One studied its behaviour

276

Design of a new serotonin receptor 5-HT_1_A imaging agent based on "9"9"mTc

Six uranyl coordination compounds, UO_2(OH)(PYCA) (1), UO_2(PYCA)_2(H_2O).2H_2O (2), UO_2(PIC)_2 (3), UO_2(H_2O)_2(NIC)_2 (4), UO_2(OH)(HINIC)(INIC) (5), and UO_2(PYTAC)_2(H_2O)_2 (6) were grown as single crystals via hydrothermal synthesis (PYCA - pyrazine-2-carboxylate, PIC - picolinate, NIC - nicotinate, INIC - iso-nicotinate, and PYTAC - 2-(pyridin-4-yl)thiazole-5-carboxylate) to study their optical properties. All six compounds have been identified via single crystal X-ray diffraction and fully characterized via powder X-ray diffraction, infrared spectroscopy, UV-Vis spectroscopy, and fluorescence spectroscopy. Three of the complexes, 1, 3, and 6, represent new structures, and their synthesis and structural characterization is detailed within. The structures of 2, 4, and 5 have previously been reported in the literature. Coordination polymer 1 crystallizes in the orthorhombic space group Pca21 (a = 13.5476(5) Angstroms, b = 6.6047(2) Angstroms, c = 8.3458(3) Angstroms), and forms ...

2011-06-01

277

Biogenic iron oxyhydroxide formation at mid-ocean ridge hydrothermal vents: Juan de Fuca Ridge

Serotonin is one of the neurotransmitters found in the brain and mediates brain functions. It is very well known that serotonin related brain abnormalities are exerted mainly via serotonin receptors in a similar manner to other neurotransmitters found in the brain. Recently, it has also been found that serotonin is involved in Alzheimer's disease either directly or indirectly by its actions on serotonergic neurons. To understand and treat the diseases caused by abnormalities in the serotonergic system in the brain, it is certain that its mechanism of function has to be well investigated. So far several 5-HT receptors and receptor subtypes have been well characterized. Moreover, serotonin agonists and antagonists acting on specific receptors are chemically synthesized and are now available for the prevention or treatment of serotonergic related diseases. In recent years, a great demand for developing neuroimaging agents has emerged for the diagnosis of abnormal brain functions in the ...

2004-07-01

278

A dinuclear Ni(I) system having a diradical Ni2N2 diamond core resting state: synthetic, structural, spectroscopic elucidation, and reductive bond splitting reactions.

Here we examine Fe speciation within Fe-encrusted biofilms formed during 2-month seafloor incubations of sulfide mineral assemblages at the Main Endeavor Segment of the Juan de Fuca Ridge. The biofilms were distributed heterogeneously across the surface of the incubated sulfide and composed primarily of particles with a twisted stalk morphology resembling those produced by some aerobic Fe-oxidizing microorganisms. Our objectives were to determine the form of biofilm-associated Fe, and identify the sulfide minerals associated with microbial growth. We used micro-focused synchrotron-radiation X-ray fluorescence mapping (mu XRF), X-ray absorption spectroscopy (mu EXAFS), and X-ray diffraction (mu XRD) in conjunction with focused ion beam (FIB) sectioning, and highresolution transmission electron microscopy (HRTEM). The chemical and mineralogical composition of an Fe-encrusted biofilm was queried at different spatial scales, and the spatial relationship between primary sulfide and ...

2008-05-22

279

Estimating the stabilities of aqueous actinide complexes with sulfoxy-anions

One-electron reduction of the square-planar nickel precursor (PNP)NiCl ( 1) (PNP (-) = N[2-P(CHMe 2) 2-4-methylphenyl] 2) with KC 8 effects ligand reorganization of the pincer ligand to assemble a Ni(I) dimer, [Ni(mu 2-PNP)] 2 ( 2), containing a Ni 2N 2 core structure, as inferred by its solid-state X-ray structure. Solution magnetization measurements are consistent with a paramagnetic Ni(I) system likely undergoing a monomer dimer equilibrium. The room-temperature and 4 K solid-state X-band electron paramagnetic resonance (EPR) spectra display anisotropic signals. Low-temperature solid-state X-band EPR data at 4 K reveal rhombic values g z = 1.980(4), g x = 2. 380(4), and g y = 2.225(4), as well as a forbidden signal at g = 4.24 for the Delta M S = 2 half field transition, in accord with 2 having two weakly interacting metal centers. Utilizing an S = 1 model, full spin Hamiltonian simulation of the low-temperature EPR spectrum on the solid ...

2008-10-15

280

{alpha}- and {beta}-Cyclodextrin [2]rotaxanes with (diethylenetriamine)platinum(II) stoppers

Full text of publication follows: Stable aqueous sulfur species are mainly sulfide (H{sub 2}S) and sulfate (SO{sub 4}{sup 2-}) ions. However, several sulfoxy-anions may be detected as metastable anions in natural environment, as typically thiosulfate (S{sub 2}O{sub 3}{sup 2-}) and sulfite (SO{sub 3}{sup 2-}) ions [1]. In natural systems, uranium speciation and migration are mainly governed by carbonate complexes in non reducing conditions. Whereas sulfate is already known as a complexing agent of actinides, data relating to U-SO{sub 3}{sup 2-} and U-S{sub 2}O{sub 3}{sup 2-} complexes have only been proposed for U(VI) [2], but are usually not included in thermodynamic databases [3]. Therefore, it appears to be relevant to determine complexation constants of actinides with sulfur ligands, for RN migration studies, concerning nuclear waste disposal as well as migration behaviour in the geosphere. In the present study, values have been estimated for the first ...

2005-07-01

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16

281

Variation in the binding of /sup 125/I-labeled interferon-beta ser to cellular receptors during growth of human renal and bladder carcinoma cells in vitro

A series of dinuclear platinum(II) complexes, [(dien)Pt(NH{sub 2}(CH{sub 2}){sub n}NH{sub 2})Pt(dien)]Cl{sub 4} (dien = diethylenetriamine, n = 8, 9, 10, and 12) and their corresponding [2]rotaxanes with {alpha}-cyclodextrin ({alpha}-CD), [(dien)Pt{l_brace}NH{sub 2}(CH{sub 2}){sub n}NH{sub 2}{center_dot}{alpha}-CD{r_brace}Pt(dien)]Cl{sub 4}, have been synthesized and characterized by {sup 1}H, {sup 13}C, and {sup 195}Pt NMR spectroscopy and electrospray mass spectrometry. The rotaxanes were prepared by reacting the {l_brace}NH{sub 2}(CH{sub 2}){sub n}NH{sub 2}{center_dot}{alpha}-CD{r_brace} pseudorotaxanes with [Pt(dien)]Cl, to stopper the included linear {alpha},{omega}-diaminoalkane chains with the inert Pt(II) end groups. The kinetics of the self-assembly and dissociation of the {beta}-CD rotaxane, [(dien)Pt{l_brace}NH{sub 2}(CH{sub 2}){sub 10}NH{sub 2}{center_dot}{beta}-CD{r_brace}Pt(dien)]{sup 4+}, were investigated by using {sup 1}H NMR and are indicative of a slippage mechanism, ...

2005-12-15

282

Theoretical study on antitumor activity of palladium(II) and platinum(II) complexes with isoxazole and its derivatives

Studies of various established human bladder and renal carcinoma cell lines cultured in vitro demonstrated the presence of specific, saturable, high affinity binding sites for /sup 125/I-labeled human interferon Beta ser IFN-beta ser). This recombinant produced interferon labeled with approximately one atom of /sup 125/I/molecule of IFN expressed minimal or no loss of antiviral activity. A single class of binding sites (1000-2000/cell) with an affinity constant of 10(10)-10(11) L/M was measured at 4 degrees C for cells exhibiting widely different sensitivity to the antiproliferative effect of IFN-beta ser. Major fluctuations in the binding of /sup 125/I-labeled IFN-beta ser to cellular receptors were observed during in vitro proliferation of four of five cell lines examined. A significant decrease (P less than 0.001) in specific binding was observed 48 h after cultures were established. Cell cycle analysis suggested that within the first 24 h and in the very late log and stationary ...

1987-09-01

283

The neuronal nicotinic acetylcholine receptor {alpha}7 subunit gene: Cloning, mapping, structure, and targeting in mouse

The palladium(II) and platinum(II)complexes(where, (M(L){sub 2}X{sub 2}), M=Pd(II), Pt(II); L=isoxazole (isox), 3, 5-dimethylisoxazole(3, 5-diMeisox), 3-methyl, 5-phenylisoxazole(3-Me, 5-Ph-isox), and 4-amino-3, 5-di-methylisoxazole (4-ADI); X=Cl, Br) with isoxazole and its derivatives were investigated on antitumor activity by MM2 and EHMO calculation. Because for all the complexes the {sigma}MO energy level (E{sub {sigma}}{sub (M-X)} between d{sub x}{sup 2}{sub -y}{sup 2} orbital of central metal and p{sub x} orbital of halogen atom is less than {sigma}MO energy level E{sub {sigma}}{sub (M-N)} between d{sub x}{sup 2}{sub -y}{sup 2} orbital of central metal and p{sub x} orbital of N atom, without exception. And judging, from the lower E{sub {sigma}}{sub (M-X)} value in trans, the bonding strength was found to be weaker in trans isomer than in cis. For the Pd(II) and Pt(II) complexes which have planar ligands, it was shown that for all the complexes dissociation of ...

1998-02-01

284

The effect of ethanol on "3"5-S-TBPS binding to mouse brain membranes in the presence of chloride

The neuronal nicotinic acetylcholine receptor {alpha}7 subunit is a member of a family of ligand-gated ion channels, and is the only subunit know to bind {alpha}-bungarotoxin in mammalian brain. {alpha}-Bungarotoxin binding sites are known to be more abundant in the hippocampus of mouse strains that are particularly sensitive to nicotine-induced seizures. The {alpha}7 receptor is highly permeable to calcium, which could suggest a role in synaptic plasticity in the nervous system. Auditory gating deficiency, an abnormal response to a second auditory stimulus, is characteristic of schizophrenia. Mouse strains that exhibit a similar gating deficit have reduced hippocampal expression of the {alpha}7 subunit. We have cloned and sequenced the full length cDNA for the mouse {alpha}7 gene (Acra-7) and characterized its gene structure. The murine {alpha}7 shares amino acid identity of 99% and 93% with the rat and human {alpha}7 subunits, respectively. Using an interspecies ...

1994-09-01

285

Synthesis, characterization and biologic effects of polybrominated naphthalenes

The effect of in vitro and in vivo administration of ethanol on the binding of "3"5S-t-butyl-bicyclophosphorothionate ("3"5S-TBPS) to cortical brain membranes of C57B1 mice was investigated using KCl (100 mM) containing assay media. The in vitro addition of ethanol produced a dose-dependent inhibition of basal "3"5S-TBPS binding. In the presence of chloride ions, GABA and pentobarbital had a biphasic action (stimulation followed by inhibition) on "3"5S-TBPS binding, whereas diazepam only stimulated the binding. Ethanol reduced the stimulatory effects of GABA and pentobarbital in a dose-dependent manner, but had no effect on the enhancement of "3"5S-TBPS binding produced by diazepam. "3"5S-TBPS binding to cortical brain membranes was inhibited by the putative Cl"- channel blocking agent DIDS. This inhibitory action of DIDS was significantly, and dose-dependently reduced by ethanol (#<=# 100 mM ethanol). Chronic ethanol ingestion in vivo, which produced tolerance to and physical ...

286

Structural and Biochemical Basis for the Binding Selectivity of Peroxisome Proliferator-activated Receptor [gamma] to PGC-1[alpha

Although polybrominated naphthalenes (PBNs) are contaminants of the commercial fire retardant fireMaster BP-6, the individual PBN isomers have not been identified. In order to study PBNs possessing an analogous level of bromination to those found in fireMaster BP-6, three synthetic PBN mixtures, averaging 5.0, 5.3, and 5.6 bromines per naphthalene were synthetized and partially characterized. The PBN mixtures were administered to immature male Wistar rats and found to be potent inducers of cytochrome P-450-dependent monooxygenases. At the lowest dose tested, 30 mumol X kg-1, each PBN mixture caused maximal induction of benzo(a)pyrene hydroxylase activity. On the basis of enzyme activities, ligand-binding spectra and sodium dodecyl sulfate-polyacrylamide gel electrophoresis, the PBN mixtures were determined to be 3-methylcholanthrene-type inducers of cytochrome P-450 (P-448), resembling qualitatively the most toxic polyhalogenated biphenyls, dibenzofurans, and ...

1984-07-01

287

Square planar platinum(II) complexes: Synthesis, IR spectroscopy, and hydration equilibrium of Pt[sup II]L(CN)[sub 2] (L = 4,4[prime]-(t-Bu)[sub 2]-2,2[prime]-bpy)

The functional interaction between the peroxisome proliferator-activated receptor {gamma} (PPAR{gamma}) and its coactivator PGC-1{alpha} is crucial for the normal physiology of PPAR{gamma} and its pharmacological response to antidiabetic treatment with rosiglitazone. Here we report the crystal structure of the PPAR{gamma} ligand-binding domain bound to rosiglitazone and to a large PGC-1{alpha} fragment that contains two LXXLL-related motifs. The structure reveals critical contacts mediated through the first LXXLL motif of PGC-1{alpha} and the PPAR{gamma} coactivator binding site. Through a combination of biochemical and structural studies, we demonstrate that the first LXXLL motif is the most potent among all nuclear receptor coactivator motifs tested, and only this motif of the two LXXLL-related motifs in PGC-1{alpha} is capable of binding to PPAR{gamma}. Our studies reveal that the strong interaction of PGC-1{alpha} and PPAR{gamma} is mediated through both ...

2008-07-23

288

Simulation of the experimental crystal field splitting pattern of a mono tetrahydrofuran adduct derived from tris(bis(trimethylsilyl)amido)neodymium(III)

The hydration behavior of a number of square planar Pt(II) bis(cyano) complexes has been examined, and the limiting stoichiometries are related to the steric requirements of the dinitrogen bidentate ligands coordinated to the metal center. In particular, the IR, UV/vis, and [sup 1]H, [sup 13]C, and [sup 195]Pt NMR spectroscopic data for the compound Pt[sup II]dtbipy(CN)[sub 2] [dtbipy = 4,4[prime]-[l brace]C(CH[sub 3])[sub 3][r brace][sub 2]-2,2[prime]-bpy] have been determined and show that, at relative humidities (rh) above [approximately]40%, this complex sorbs five water molecules at room temperature. The sorption process consists of a rapid step in which one H[sub 2]O adds to the complex and which appears to be independent of rh, followed by a slower, rh-dependent step leading to the final stoichiometry. In contrast, the analogous 2,2[prime]-bpy complex sorbs no water under these conditions, while the 4,4[prime]-(CH[sub 3])[sub 2]-2,2[prime]-bpy complex sorbs ...

1992-12-23

289

Raman Under Nitrogen. The High-Resolution Raman Spectroscopy of Crystalline Uranocene, Thorocene, and Ferrocene

Full text: In case of lanthanide (Ln) compounds the bis(trimethylsilyl)amido (btmsa) ligand is considered as a steric and electronic equivalent of the bis(trimethylsilyl)methanido (btmsm) group . Because of their extreme air and moisture sensitivity the chemistry of Ln(btmsm)_3 is very poor, whereas that of comparatively stable Ln(btmsa)_3 is much more developed. As we wish to extend the chemistry of Ln(btmsm)_3 and plan to derive and to parameterize the crystal field (CF) splitting patterns of the target molecules, it is recommended to study in advance the electronic structures of the corresponding compounds derived from Ln(btmsa)_3 . Beside (btmsa)_3 Nd(m-Cl)Li(THF)_3 a number of mono base adducts [(btmsa)_3 Ln.B] with sterically less demanding bases such as OPPh_3 , NCtBu or CNtBu have been described and were partly structurally characterized. Considering only the immediately coordinating atoms, the effective CF is of C_3_v symmetry. According to recent ...

1998-10-25

290

Raman Under Nitrogen. The High-Resolution Raman Spectroscopy of Crystalline Uranocene, Thorocene, and Ferrocene

The utility of recording Raman spectroscopy under liquid nitrogen, a technique we call Raman Under Nitrogen (RUN), is demonstrated for ferrocene, uranocene and thorocene. Using RUN, low temperature (liquid nitrogen cooled) Raman spectra for these compounds exhibit higher resolution than previous studies and new vibrational features are reported. The first Raman spectra of crystalline uranocene at 77 K are reported using excitation from argon (5145 ) and krypton (6764 ) ion lasers. The spectra obtained showed bands corresponding to vibrational transitions at 212, 236, 259, 379, 753, 897, 1500, and 3042 cm-1 , assigned to ring-metal-ring stretching, ring-metal tilting, out-of-plane CCC bending, in-plane CCC bending, ring-breathing, C-H bending, CC stretching and CH stretching, respectively. The assigned vibrational bands are compared to those of uranocene in THF and thorocene. All vibrational frequencies of the ligands, except the 259 cm-1 out-of-plane CCC bending ...

2004-02-08

291

Prevention of physostigmine-, DFP-, and diazinon-induced acute toxicity by monoethylcholine and N-aminodeanol.

2004-02-08

292

Preparation and biodistribution of yttrium-90 lipiodol in rats following hepatic arterial injection

1. Choline, and the choline analogues monoethylcholine (MEC) and N-aminodeanol (NAD) were examined for prophylactic activity in acute acetylcholinesterase inhibitor toxicity in mice. The rank order of potency of the compounds was MEC greater than NAD greater than choline. 2. Simultaneous administration of MEC (60 mg kg-1) or NAD (200 mg kg-1) with physostigmine reduced lethality to 17 and 13% respectively. MEC (60 mg kg-1) completely protected against disopropylfluorophosphate (DFP) and diazinon toxicity, and NAD reduced lethality to 17% for both agents. Choline (200 mg kg-1) exhibited only negligible antidotal activity against the inhibitors. 3. In vitro concentrations of choline, MEC, and NAD, similar to the estimated concentration obtained in vivo in the acute toxicity study, produced mixed inhibition of mouse brain acetylcholinesterase. The inhibition was dose-related and was additive to the inhibition produced by the cholinesterase inhibitors. 4. All three analogues reduced ...

1989-06-01

293

Organic light-emitting devices based on solution-processible quinolato-complex supramolecules

We labelled Lipiodol with yttrium-90 and analysed the biodistribution in rats after intrahepatic arterial injection. An RP-18 column was used to separate {sup 90}Y from strontium-90. {sup 90}Y was retained on the column, which had been pretreated with yttrium-selective extraction reagent, di(2-ethylhexyl) phosphate, while {sup 90}Sr was washed out. A hexadentate nitrogen-donor chelating ligand N,N,N`,N`-tetrakis(2-benzymidazolylmethyl)-1,2-ethanediamine (EDTB) was synthesized by condensation of 1,2-benzenediamine and ethylene diamine tetra-acetic acid (EDTA). Lipiodol was covalently conjugated with EDTB. The final product was obtained by eluting the retained {sup 90}Y from the RP-18 column with EDTB-Lipiodol. Sixteen male rats (Sprague-Dawley) were sacrificed at 1 h, 24 h, 48 h and 72 h (four rats at each time) after injection of approximately 0.1 mCi {sup 90}Y-Lipiodol via the hepatic artery. Samples of liver, spleen, muscle, lung, kidney, bone, whole blood and ...

1995-03-01

294

Novel bifunctional natriuretic peptides as potential therapeutics.

This paper discusses a new type of supramolecular material tris{5-N-[3-(9H-carbazol-9-yl)propyl]-N-(4-methylphenyl) aminesulfonyl-8-hydroxyquinolato} aluminum(III), Al(SCarq)3, which we synthesized using three 5-N-[3-(9H-carbazol-9-yl)propyl]-N-(4-methylphenyl) aminesulfonyl-8-hydroxyquinoline as bidentate ligands. The peak photoluminescence in the solid phase appears at 488 nm. In cyclic voltammetric measurement, two oxidation peaks, which were obtained at -5.6 and -5.9 eV, correspond to HOMO sites of carbazoyl and aluminum quinolates, respectively. In the investigation of solid morphological thin film, the flat surface was investigated using an atomic force microscope. The root mean square (rms) and mean roughness (Ra) were respectively measured to be 0.427 and 0.343 nm. For the fabrication of organic light-emitting devices (OLEDs) using spin-coating techniques, the turn-on voltage and maximum luminescence of the optimized electroluminescence device, glass/ITO ...

2009-02-15

295

Nod2 sensing of lysozyme-digested peptidoglycan promotes macrophage recruitment and clearance of S. pneumoniae colonization in mice.

Synthetic atrial natriuretic peptide (carperitide) and B-type natriuretic peptide (BNP; nesiritide) are used to treat congestive heart failure. However, despite beneficial cardiac unloading properties, reductions in renal perfusion pressures limit their clinical effectiveness. Recently, CD-NP, a chimeric peptide composed of C-type natriuretic peptide (CNP) fused to the C-terminal tail of Dendroaspis natriuretic peptide (DNP), was shown to be more glomerular filtration rate-enhancing than BNP in dogs. However, the molecular basis for the increased responsiveness was not determined. Here, we show that the DNP tail has a striking effect on CNP, converting it from a non-agonist to a partial agonist of natriuretic peptide receptor (NPR)-A while maintaining the ability to activate NPR-B. This effect is specific for human receptors because CD-NP was only a slightly better activator of rat NPR-A due to the promiscuous nature of CNP in this species. Interesting, the DNP tail alone had no effect ...

2008-10-21

296

Kinetics of in vivo binding of antagonist to muscarinic cholinergic receptor in the human heart studied by Positron Emission Tomography

Streptococcus pneumoniae colonizes the mucosal surface of the human upper respiratory tract. A colonization event is gradually cleared through phagocytosis by monocytes/macrophages that are recruited to the airway lumen. Here, we sought to define the bacterial and host factors that promote monocyte/macrophage influx and S. pneumoniae clearance using intranasal bacterial challenge in mice. We found that the recruitment of monocytes/macrophages required their expression of the chemokine receptor CCR2 and correlated with expression of the CCR2 ligand CCL2. Production of CCL2 and monocyte/macrophage recruitment were deficient in mice lacking digestion of peptidoglycan by lysozyme (LysM) and cytosolic sensing of the products of digestion by Nod2. Ex vivo macrophages produced CCL2 following bacterial uptake, digestion by LysM, and sensing of peptidoglycan by Nod2. Sensing of digested peptidoglycan by Nod2 also required the pore-forming toxin pneumolysin. The generation ...

2011-08-15

297

Kinetic analysis of transport and opioid receptor binding of ( sup 3 H)(-)-cyclofoxy in rat brain in vivo: Implications for human studies

Positron Emission Tomography (PET) was used to analyze in vivo antagonist binding to human myocardial muscarinic cholinergic receptor. The methiodide salt of the muscarinic antagonist, quinuclidinyl benzilate (MQNB), was labeled with the positron emitter, Carbon-11, and injected intravenously to 8 normal subjects. /sup 11/C-MQNB concentration was determined in vivo in the ventricular septum from 40 cross-sectional images acquired at the same transverse level over a period of 70 minutes. In 4 subjects, various amounts of unlabeled atropine were rapidly injected at 20 minutes to study whether atropine competitively inhibited MQNB. The kinetics of binding of /sup 11/C-MQNB were not the same in vivo and in vitro. The apparent dissociation rate of /sup 11/C-MQNB in vivo was much slower (by 1 to 2 orders of magnitude) than that observed in vitro with /sup 3/H-QNB. After atropine injection, /sup 11/C-MQNB dissociated from its binding sites at a rate that apparently depended on the amount of ...

1984-08-27

298

Isoelectric focusing purity criteria and "1H NMR detectable spectroscopic heterogeneity in the major isolated monomer hemoglobins from Glycera dibranchiata

(3H)Cyclofoxy (CF: 17-cyclopropylmethyl-3,14-dihydroxy-4,5-alpha-epoxy-6-beta-fluoromorp hinan) is an opioid antagonist with affinity to both mu and kappa subtypes that was synthesized for quantitative evaluation of opioid receptor binding in vivo. Two sets of experiments in rats were analyzed. The first involved determining the metabolite-corrected blood concentration and tissue distribution of CF in brain 1 to 60 min after i.v. bolus injection. The second involved measuring brain washout for 15 to 120 s following intracarotid artery injection of CF. A physiologically based model and a classical compartmental pharmacokinetic model were compared. The models included different assumptions for transport across the blood-brain barrier (BBB); estimates of nonspecific tissue binding and specific binding to a single opiate receptor site were found to be essentially the same with both models. The nonspecific binding equilibrium constant varied modestly in different brain structures (Keq = ...

1991-03-01

299

High-affinity lead binding proteins in rat kidney cytosol mediate cell-free nuclear translocation of lead

Three major monomeric hemoglobins have been isolated from the erythrocytes of Glycera dibranchiata. Their importance to structure-function studies of heme proteins lies in the fact that they have been shown to possess an exceptional amino acid substitution. In these proteins, the E-7 position is occupied by leucine rather than the more common distal histidine. This substitution alters the polarity of the heme ligand binding environment compared to myoglobin. Due to this, the G. dibranchiata monomer hemoglobins are attracting much attention. However, until now no purity criterion has been developed. Here the authors demonstrate that, for all of the Glycera momomer hemoglobins, multiple line patterns are shown on high-voltage isoelectric focusing (IEF) gels. Most of these lines are shown to be a consequence of heme-related phenomena and can be understood on the basis of changes in oxidation and ligation state of the heme iron. The multiple line pattern does not ...

300

High-affinity lead binding proteins in rat kidney cytosol mediate cell-free nuclear translocation of lead

The PbII binding characteristics of the previously reported PbII binding proteins of rat kidney cytosol were investigated further. Saturation and Scatchard analysis of /sup 203/Pb binding in whole cytosol and in 40% saturated ammonium sulfate precipitated fractions disclosed a class of relatively high-affinity sites with an apparent Kd of approximately 50 nM and binding capacities of approximately 41 and 9 pmol/mg of protein, respectively. Two /sup 203/Pb binding proteins with approximate molecular masses of 63K and 11.5K daltons and a high molecular weight component (greater than 200K) were isolated by Sepharose-6B column chromatography. The time course of association of /sup 203/Pb with cytosol and the 63K protein showed maximum binding at 18 hr which was stable up to 25 hr at 4 degrees C. The approximate half-time dissociation rate (T 1/2) of specifically bound /sup 203/Pb to the 63K protein was 100 min at 4 degrees C whereas the 11.5K protein showed little dissociation of ...

1985-02-01

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16

301

High-Performance, Superparamagnetic, Nanoparticle-Based Heavy Metal Sorbents for Removal of Contaminants from Natural Waters

The PbII binding characteristics of the previously reported PbII binding proteins of rat kidney cytosol were investigated further. Saturation and Scatchard analysis of "2"0"3Pb binding in whole cytosol and in 40% saturated ammonium sulfate precipitated fractions disclosed a class of relatively high-affinity sites with an apparent Kd of approximately 50 nM and binding capacities of approximately 41 and 9 pmol/mg of protein, respectively. Two "2"0"3Pb binding proteins with approximate molecular masses of 63K and 11.5K daltons and a high molecular weight component (greater than 200K) were isolated by Sepharose-6B column chromatography. The time course of association of "2"0"3Pb with cytosol and the 63K protein showed maximum binding at 18 hr which was stable up to 25 hr at 4 degrees C. The approximate half-time dissociation rate (T 1/2) of specifically bound "2"0"3Pb to the 63K protein was 100 min at 4 degrees C whereas the 11.5K protein showed little dissociation of specifically bound ...

302

Fluoride complexes of Pt(II) as nucleophiles: activity of PtCl/sub 4//sup 2 -/, PtCl/sub 3/(H/sub 2/O)/sup -/, and PtCl/sub 3/(C/sub 2/H/sub 4/)/sup -/ anions in the oxidative addition of methyl iodide

We describe the synthesis and characterization of superparamagnetic iron oxide nanoparticle based heavy metal sorbents with various surface chemistries that demonstrate an excellent affinity for the separation of heavy metals in contaminated water systems (i.e. spiked Columbia river water). The magnetic nanoparticle sorbents are prepared from an easy to synthesize iron oxide precursor, followed by a simple, one-step ligand exchange technique to introduce the organic surface functionality of interest chosen to target either specific or broader classes of heavy metals. Functionalized superparamagnetic nanoparticles are excellent sorbent materials for the extraction of heavy metal contaminants from environmental and clinical samples since they are easily removed from the media once bound to the contaminant by simply applying a magnetic field. These engineered magnetic nanoparticle sorbents have an inherently high active surface area (often > 100 m2/g), allowing for ...

2010-06-01

303

Experimental study on the absorption behaviors of gas phase bivalent mercury in Ca-based wet flue gas desulfurization slurry system.

The kinetics of the oxidative addition of CH/sub 3/I to platinum(II) complexes in aqueous solutions of K/sub 2/PtCl/sub 4/ and KPtCl/sub 3/(C/sub 2/H/sub 4/) have been studied by PMR and GLC. The second-order rate constants for the PtCl/sub 3/(H/sub 2/O)/sup -/ and PtCl/sub 4//sup 2 -/ particles are equal to 400 exp(-2.7 x 10/sup 3//T) and 3.18 x 10/sup 10/ exp(-9.2 x 10/sup 3//T) mole/sup -1/ x liter x sec/sup -1/, respectively. The introduction of a ..pi..-acceptor ligand, viz. ethylene, into the coordination sphere of platinum(II) results in a sharp drop in the rate, probably due to a decrease in the electron density on the platinum atom. According to the PMR data, the product of the oxidative addition of CH/sub 3/I to Zeise's salt is a methyl complex of platinum(IV), is identical to the complex obtained by reacting methyl iodide with K/sub 2/PtCL/sub 4/, and does not contain an olefin.

1987-05-01

304

Distribution of lead-203 in human peripheral blood in vitro

Gas phase oxidation and catalytic oxidation of element mercury (Hg(0)) to bivalent mercury (Hg(2+)) were proposed to improve the mercury removal efficiency in the wet flue gas desulfurization (WFGD) system. However, the re-emission of Hg(0), generated by the reduction of absorbed Hg(2+), would lead to a damping of the total mercury removal efficiency. In this paper, the absorption and reduction behaviors of bivalent mercury in the Ca-based WFGD slurry were evaluated in our purpose-built device. According to our experimental results, the slurry chemistry (such as CaSO(3) content, SO(4)(2-), Cl(-) and pH value) had a strong influence on the reduction of absorbed bivalent mercury. And the inlet concentrations of SO(2) and O(2) contribute little to the mercury absorption. Within the typical pH value range of 4.5-5.5, about 70% of inlet bivalent mercury was converted to Hg(0). The re-emission of Hg would be greatly retarded with the increase of [SO(4)(2-)] due to the formation of HgSO(4) or ...

2010-08-06

305

Development of a new radiolabel (lead-203) and new chelating agents for labeling monoclonal anntibodies for imaging

In-vitro experiments using "2"0"3Pb were performed to identify the lead binding components in human peripheral blood. The distribution of lead in plasma, in the red cell membrane, and within the red cell was also investigated. Studies of the distribution of "2"0"3Pb in the whole blood showed that at a lead concentration of 2.45 #mu#mol/l (50 #mu#g/100 ml) about 94% of lead had been incorporated by the erythrocytes and 6% remained in the plasma. After extraction of lipid by a methanol/chloroform mixture, about 75% of the lead was found to be associated with the protein fraction. The lipid contained about 21% of the "2"0"3Pb, the remainder being in the aqueous plasma. SDS polyacrylamide gel electrophoresis of blood plasma showed that almost 90% of the "2"0"3Pb was present in the albumin fraction; the remainder was likely to be associated with high molecular weight globulins. Several binding sites were identified on the erythrocyte membrane. The high molecular weight component, about 130 ...

306

Curious Results with Palladium- and Platinum-Carrying Polymers in Mass Cytometry Bioassays and an Unexpected Application as a Dead Cell Stain.

High liver uptake and slow body clearance presently limit the usefulness of "1"1"1In labeled antibodies for tumor imaging. We have investigated "2"0"3Pb as an alternate and better antibody label. The DTPA and cyclohexyl EDTA (CDTA) conjugates of an anticolon carcinoma antibody, 17-1A were labeled (bicyclic anhydride method) with "2"0"3Pb and "1"1"1In with 60 and 90% labeling yields, respectively. The biodistribution of "2"0"3Pb-17-1A conjugates was compared with the corresponding "1"1"1In-labeled preparations and with "2"0"3Pb-DTPA, "2"0"3Pb-nitrate and nonrelevant antibody controls in normal and human tumor (SW948) xenografted nude mice at 24, and 96 hr. Lead-203-labeled CDTA and DTPA antibody conjugates gave similar in vivo distributions. Even though the lead bound to these chelate-antibody conjugates was more labile in serum and in vivo, compared to indium, it cleared much faster from the liver and the whole body. A new series of chelating agents based on the incorporation of a ...

1988-05-22

307

Comparison of radiationless decay processes in osmium and platinum porphyrins

We describe the synthesis of metal-chelating polymers (MCPs) with four different pendant polyaminocarboxylate ligands (EDTA, DTPA, TTHA, DOTA) and an orthogonal end-group, either a fluorescein molecule or a bismaleimide linker for antibody attachment. Polymer characterization by a combination of (1)H NMR, UV/vis absorption measurements, and thermal gravimetric analysis (TGA) indicated that each chain of the fluorescein-terminated polymers contained one dye molecule. These polymer samples were loaded with three different types of lanthanide ions as well as palladium and platinum ions. The numbers of metal atoms per chain were determined by a combination of UV/vis and conventional ICP-MS measurements. The experiments with lanthanide ions demonstrated that a net anionic charge on the polymer is important for water solubility. These experiments also showed that at least one type of lanthanide ion (La(3+)) is capable of forming a bimetallic complex with pendant DTPA ...

2011-09-28

308

Characterization of histamine H_1-receptor binding peptides in guinea pig brain using ["1"2"5I]iodoazidophenpyramine, an irreversible specific photoaffinity probe

Two osmium porphyrin complexes, Os(OEP)L_2 [OEP = octaethylporphin, L = py(pyridine) or NO], and PtOEP were investigated by picosecond laser spectroscopy with use of a double-beam, mode-locked Nd:glass system delivering 6-ps (fwhm) pulses at 527 nm with 1-2mJ/pulse. Time-resolved excited-state spectra were recorded from the time of photoexcitation to 5 ns after photoexcitation. The initial excited state, S_1, decayed in less than or equal to9 ps for the two osmium complexes and in less than or equal to15 ps for the platinum porphyrin. A second excited state, T_1, lived for 1, 9, and >50 ns respectively for Os(OEP)(py)_2, Os(OEP)(NO)_2, and PtOEP. The #DELTA#A spectra of the T_1 states of the osmium complexes were similar to those of previously reported (d/sub #pi#/,#pi#*) states for Os(OEP)(py)_2 and (#pi#,#pi#*) states for Os(OEP)(NO)_2. This finding supports prior assignments of these states on the basis of expected axial and equatorial back-bonding of the osmium's d electrons. ...

309

Characterization and properties of monoammine nitroimidazole complexes of platinum (PtCl sub 2 (NH sub 3 )(NO sub 2 Im)). Crystal and molecular structure of cis-Amminedichloro(1-((((2-hydroxyethyl)amino)carbonyl)methyl)-2-nitroimidazole)platinum(II)

Aminophenpyramine, a derivative of mepyramine (pyrilamine), a typical antagonists of histamine at its H_1 receptor was synthesized and converted into ["1"2"5I]iodoazidophenpyramine, a potential photoaffinity probe for the H_1 receptor. In the dark, reversible binding of this probe to cerebellar membranes occurred with a K/sub d/ of 1.2 x 10"-"1"1 M and a B/sub max/ of 240 fmol/mg of protein and was inhibited by various H_1-receptor antagonists with the expected potencies. These features establish the compound as one of the most potent H_1-receptor antagonists known so far. Upon IV irradiation, 5% of the bound radioactivity was covalently incorporated into cerebellar membrane polypeptides as shown by standard NaDodSO_4/PAGE. Two bands of 47 and 56 kDa were consistently labeled, labeling being prevented by various H_1-receptor antagonists with the expected potencies and stereoselectivity. In the presence of protease inhibitors, labeling of the 56-kDa peptide increased at the expense of ...

310

"1H and "3"1P nuclear magnetic resonance investigation of the interaction between 2,3-diphosphoglycerate and human normal adult hemoglobin

The characterization of monoammine(nitroimidazole)platinum(II) complexes of structure (PtCl{sub 2}(NH{sub 3})(NO{sub 2}Im)) (NO{sub 2}Im = 1-((((2-hydroxyethyl)amino)carbonyl)methyl)-2-nitroimidazole, Etanidazole (I), 1-(2-nitro-1-imidazolyl)-3-methoxy2-propanol, Misonidazole (II), and 1-(2-hydroxyethyl)-2-methyl-5-nitroimidazole, Metronidazole (III)) is reported. Both is cis and trans isomers may be isolated for II and III. The crystal structure of cis-amminedichloro(1-((((2-hydroxyethyl)amino)carbonyl)methyl)-2-nitroimidazole)platinum(II) has been determined by X-ray diffraction. The crystals are orthorhombic, space group Pnab with cell dimensions a = 14.867 (7) {angstrom}, b = 9.915 (5) {angstrom}, c = 19.015 (9) {angstrom}, and Z = 8. The structure was refined to R = 0.062 and R{sub w} = 0.052. Platinum has the expected square-planar coordination. The Pt-Cl bond trans to the nitroimidazole ligand is shorter (2.269 (3) {angstrom}) than normal. The dihedral angle ...

1991-11-27

311

Carbomolybdates(III): On Pr{sub 2}[Mo{sub 2}C{sub 3}] and structural relations to Er{sub 2}Mo{sub 2}C{sub 3}; Carbomolybdate(III): Zur Kenntnis von Pr{sub 2}[Mo{sub 2}C{sub 3}] sowie Strukturbeziehungen zu Er{sub 2}Mo{sub 2}C{sub 3}

High-resolution "1H and "3"1P nuclear magnetic resonance spectroscopy has been used to investigate the binding of 2,3-diphosphoglycerate to human normal adult hemoglobin and the molecular interactions involved in the allosteric effect of the 2,3-diphosphoglycerate molecule on hemoglobin. Individual hydrogen ion NMR titration curves have been obtained for 22-26 histidyl residues of hemoglobin and for each phosphate group of 2,3-diphosphoglycerate with hemoglobin in both the deoxy and carbonmonoxy forms. The results indicate that 2,3-diphosphoglycerate binds to deoxyhemoglobin at the central cavity between the two #beta# chains and the binding involves the #beta#2-histidyl residues. Moreover, the results suggest that the binding site of 2,3-diphosphoglycerate to carbonmonoxyhemoglobin contains the same (or at least some of the same) amino acid residues responsible for binding in the deoxy form. As a result of the specific interactions with 2,3-diphosphoglycerate, the #beta#2-histidyl ...

312

Synthesis, crystal structures and spectroscopic properties of RbBaTaS{sub 4} and K{sub 2}BaTa{sub 2}S{sub 11}

Pr{sub 2}[Mo{sub 2}C{sub 3}] was obtained by arc melting of the elements followed by annealing at 1500 C in arc welded and sealed Mo-ampoules. The compound was characterised by chemical analyses, X-ray diffraction and metallography. The crystal structure (monoclinic, P2{sub 1}/c, Z = 4, a = 597.99(10) pm, b = 665.15(11) pm, c = 1185.60(19) pm and {beta} = 111.631(5) ) represents a new structure type containing a three dimensional polyanion {sub {infinity}}{sup 3}[(Mo{sub 2}C{sub 3}){sup 6-}] with Molybdenum(III) in a distorted tetrahedral coordination by carbo-ligands. Tetrameric building-blocks, Mo{sub 4}C{sub 10}, of edge sharing MoC{sub 4}-tetrahedra are arranged to form layers running parallel to (100). The layers are interconnected along [100] by sharing common apices of the MoC{sub 4} tetrahedra. The coordination polyhedra around praseodymium represent distorted (PrC{sub 5})-arrangements (mono capped tetrahedra and square pyramids). The metal atoms together ...

2004-11-01

313

Modulation of neuronal differentiation by CD40 isoforms

Single crystals of RbBaTaS{sub 4} (1) and K{sub 2}BaTa{sub 2}S{sub 11} (2) were obtained from the reactions of Ta, with in situ formed fluxes of A{sub 2}S{sub 3} (A = K, Rb), BaS, and S at 500 C. Compound 1 crystallizes in the orthorhombic space group Pnma with a = 9.3286(5), b = 7.0391(4), c = 12.4365(7) A, V = 816.6(1) A{sup 3}, Z = 4. Compound 2 crystallizes in the monoclinic space group P2{sub 1}/c with a = 14.5280(10), b = 12.6347(7), c = 17.5148(12) A, {beta} = 94.744(8) , V = 3203.9(4) A{sup 3}, Z = 4. The structure of RbBaTaS{sub 4} (1) consists of isolated tetrahedral [TaS{sub 4}]{sup 3-} anions and Rb{sup +} and Ba{sup 2+} cations. The Ba{sup 2+} cations are surrounded by nine sulfur atoms forming distorted tricapped trigonal prisms, whereas the Rb{sup +} cations are in an irregular environment of ten sulfur atoms. The structure of K{sub 2}BaTa{sub 2}S{sub 11} (2) consists of two different dinuclear [Ta{sub 2}S{sub 11}] units which are separated by Ba{sup 2+} and K{sup +} ...

2010-10-15

314

Investigation into {sup 64}Cu-labeled Bis(selenosemicarbazone) and Bis(thiosemicarbazone) complexes as hypoxia imaging agents

Neuron differentiation is a complex process involving various cell-cell interactions, and multiple signaling pathways. We showed previously that CD40 is expressed and functional on mouse and human neurons. In neurons, ligation of CD40 protects against serum withdrawal-induced injury and plays a role in survival and differentiation. CD40 deficient mice display neuron dysfunction, aberrant neuron morphologic changes, and associated gross brain abnormalities. Previous studies by Tone and colleagues suggested that five isoforms of CD40 exist with two predominant isoforms expressed in humans: signal-transducible CD40 type I and a C-terminal truncated, non-signal-transducible CD40 type II. We hypothesized that differential expression of CD40 isoform type I and type II in neurons may modulate neuron differentiation. Results show that adult wild-type, and CD40"-"/"- deficient mice predominantly express CD40 type I and II isoforms. Whereas adult wild-type mice express mostly CD40 type I in ...

2008-05-02

315

In vivo and in vitro evaluation of dota-lanreotide radiolabelled with gallium-67

Background: Cu-diacetyl-bis(N{sup 4}-methylthiosemicarbazone) [Cu-ATSM], although excellent for oncology applications, may not be suitable for delineating cardiovascular or neurological hypoxia. For this reason, new Cu hypoxia positron emission tomography (PET) imaging agents are being examined to search for a higher selectivity for hypoxic or ischemic tissue at higher oxygen concentrations found in these tissues. Two approaches are to increase alkylation or to replace the sulfur atoms with selenium, resulting in the formation of selenosemicarbazones. Methods: Three {sup 64}Cu-labeled selenosemicarbazone complexes were synthesized and one was screened for hypoxia selectivity in vitro using EMT-6 mouse mammary carcinoma cells. Rodent biodistribution and small animal PET images were obtained from BALB/c mice implanted with EMT-6 tumors. One alkylated thiosemicarbazone was synthesized and examined. Results: Of the three bis(selenosemicarbazone) ligands synthesized and ...

2005-02-01

316

Coordination of U"4"+ in the complex U(P_2W_1_7O_6_1)"1"6"-_2 in solid state and in aqueous solution

One of the refinements of modern Nuclear Medicine is the capacity of providing dynamic and kinetics images of the administered radiopharmaceutical, reproducing its transport mechanism, action sites, receptor binding and excretion route. With the continues technological advances new radiopharmaceuticals have been developed in order to express higher specificity and with higher characters of affinity between receptor/complex. One radiopharmaceutical is formed by a reagent or bio molecule that has in its structure a radioisotope, that has the objectives of carrying it to the organs of affinity or to benign or malign tumoral process. Somatostatin inhibits the growing and proliferation of several tumoral cells. Somatostatin analogs bind to somatostatic receptors that are expressed in different kind of neoplasia DOTA-LANREOTIDE (DOTALAN) is an octapeptide analog to somatostatin. The interest of labeling the bio conjugate with gallium-67 in Nuclear Medicine comes from its physical, chemical ...

317

Carbon-carbon bond formation in cationic aryl-olefin-platinum (II) complexes

The aim of this work is to understand the reasons for the selectivity shown in the complexation by unsaturated heteropolyanions (HPA) of actinides (An) which are oxidized to the number +IV. Different studies have been carried out, both in solution and in solid state, on P_2W_1_7O_6_1"1"0"- and its complexes with Zn"2"+, UO_2"2"+, Ce"4"+, Th"4"+ and U"4"+ to characterize the nature of the complexation site offered to the cation. Among the actinides(IV), the U"4"+ ion has been selected due to its singular spectroscopic and magnetic properties. An initial series of studies, in solution, using NMR"3"1P has thus enabled us to characterize these complexes and to compare them to those formed with the complexing agent PW_1_1O_3_9"8"-. This body of data allows to identify an identical complexation site for both ligands. An analysis of the NMR"3"1P spectrum of U(P_2W_1_7O_6_1)_2"1"6"- has shown a plane of symmetry passing through the actinide and enables us to confirm the ...

1996-09-01

318

Agonist-directed trafficking of signalling at serotonin 5-HT2A, 5-HT2B and 5-HT2C-VSV receptors mediated Gq/11 activation and calcium mobilisation in CHO cells.

Cationic five-coordinate [Pt(3-R{sup 1}-4-R{sup 2}-C{sub 6}H{sub 3})(MeCN) (6-Me-py-2-CH=NPh)(C{sub 2}H{sub 4})]{sup +} complexes (R{sup 1}, R{sup 2} = H, Me, OMe) undergo an unexpected rearrangement at 0{degrees}C in chloroform solution, affording, after treatment with aqueous LiCl, the neutral four-coordinate species [Pt(2-Et-4-R{sup 1}-5-R{sup 2}-C{sub 6}H{sub 2})Cl(6-Me-py-1-CH=NPh)]. Pt-C{sub aryl} bond breaking and making is involved in the whole process, resulting in a 1,2-shift of the platinum atom to an adjacent position of the benzene ring. The same compound is obtained, together with products deriving from a typical insertion, when an equimolar amount of ethylene is added to a chloroform solution of [Pt(3-R{sub 1}-4-R{sup 2}-C{sub 6}H{sub 3})(MeCN)(6-Me-py-2-CH=NPh)]{sup +} at 0{degrees}C. When higher ethylene/Pt ratios are used, only five-coordinate [Pt(3-R{sup 1}-4-R{sup 2}-C{sub 6}H{sub 3}CH{sub 2}CH{sub 2})Cl(6-Me-py-2-CH{double_bond}NPh)(C{sub 2}H{sub 4})] complex is ...

1992-11-01

319

Hydration of swelling clay and bacteria interaction. An experimental in situ reaction study; Hydratation des argiles gonflantes et influence des bacteries. Etude experimentale de reaction in situ

Several examples of agonist-directed trafficking of receptor signalling at 5-HT2A and 5-HT2C receptors have been reported that involve independent downstream transduction pathways. We now report the functional selectivity of a series of chemically diverse agonists at human (h)5-HT2A, h5-HT2B and h5-HT2C-VSV by examining two related responses, the upstream activation of Gq/11 proteins in comparison with its associated cascade of calcium mobilisation. At the h5-HT2A receptor, d-lysergic acid diethylamide (LSD) and the antiparkinsonian agents lisuride, bromocriptine and pergolide exhibit a higher potency for Gq/11 activation than calcium release in contrast with all the other tested ligands such as 5-HT, mCPP and BW723C86, that show an opposite preference of signalling pathway. Comparable observations are made at h5-HT2B and h5-HT2C-VSV receptors, suggesting a similar mechanism of functional selectivity for the three serotonin receptors. Interestingly, the ...

2008-07-30

320