BackgroundExpansion of aquaculture is seriously limited by reductions in fish oil (FO) supply for aquafeeds. Terrestrial alternatives such as vegetable oils (VO) have been investigated...Full Text Available
Iodine-125 labelled vinyl and aryl iodides are formed via the reaction of sodium iodide-125 with vinyl- and arylboronic acids. Good yields of isomerically pure products are obtained.
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
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
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
This patent describes a process for preparing poly(aryl ether ketones) by nucleophilic displacement polymerization in the presence of at least one alkali metal base selected from potassium, rubidium or cesium, and fluoride ions, which comprises adding to the polymerization: (a) an effective amount of at least one metal salt selected from lithium, sodium, alkaline earth or lanthanide chloride, bromide, iodide, sulfate, alkyl or aryl carboxylate, cyanide, borate or phosphate to slow or stop advancement of molecular weight and (b) an end-capping agent.
1. Amino acid sequences covering the region between residues 173 and 248 [adopting the numbering system proposed by Lai, Nakai & Chang (1974) Science 183, 1204-1206] were derived for trout (Salmo...Full Text Available
Some new 3-piperazinylmethyl-5-aryl-1H-1,2,4-triazoles have been prepared and tested for their antifungal and antimicrobial activity. Among them, compounds 3g and 3h exhibited higher antifungal activity than ketoconazole against Cladosporium cladosporoides and Aspergillus niger respectively. PMID:9825120
It has been postulated that fetal vascular abnormalities in aryl hydrocarbon receptor null (ahr−/−) mice may alter cardiovascular homeostasis in adulthood....Full Text Available
BackgroundCancer stem cells (CSCs) have increased resistance to cancer chemotherapy. They can be enriched as drug-surviving CSCs (D-CSCs) by growth with chemotherapeutic drugs, and/or...Full Text Available
BackgroundCentrosome aberrations can cause genomic instability and correlate with malignant progression in common human malignancies such as breast and prostate cancer. Deregulation...Full Text Available
Chapter one is a review of the relevant literature. In chapter two the coordination chemistry of biphenyl-tailed terpyridines with octahedral metal dications is investigated. The effect of different metal ions on their aggregation modes in the solid state is also investigated. In chapter three the coordination chemistry of polyaryl-tailed terpyridines with octahedral metal dications is investigated. The effect of different aryl tails on their aggregation modes in the solid state is investigated. In chapter four the pi-pi aggregation of molecular boxes through biphenyl tails is studied. In chapter five the immobilisation of aryl tailed complexes into polyelectrolyte films has been investigated, and the arrangement of these complexes in the films has been compared with same complexes in the crystal, thus moving from three dimensional aggregation to two dimensions.
Unsymmetric diaryl alkynes were synthesized from the palladium-catalyzed decarboxylative coupling of aryl halides and propiolic acid using a continuous flow reaction system. This flow chemistry system continuously gave the desired products in moderate to good yields, and produced less byproduct than was formed in the batch reaction.
A novel, one-pot, multicomponent synthesis of 4-arylidene-3-methyl-1-(4-arylthiazol-2-yl)-1H-pyrazol-5(4H)-ones is described using phenacyl bromides, thiosemicarbazide, ethylacetoacetate, and aryl aldehydes. This synthesis involves simultaneous formation of two heterocycles like thiazole and pyrazolone along with condensation of active methylene group by aldehydes via Knoevenagel reaction. The methodology is mild, efficient, and high yielding. GRAPHICAL ABSTRACT[image omitted
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.
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 ...
The factors affecting the rate of silica leaching in alkaline aqueous media from surface silanized, nanoporous, amorphous, silica gels and from silanized silica gels that have been modified with polyamines to form the previously reported silica polyamine composites (SPCs), BP-1 and BP-2 have been investigated. Silanization with alkyl trichlorosilanes slows the rate of silica leaching relative to the unmodified silica gels. The use of bulkier aryl silanes somewhat decreases the silica leaching under the same conditions. Interestingly, after modification of the silanized silica with poly(allylamine) (PAA) to make BP-1, the leaching increases, but subsequent modification of the SPC with chloroacetic acid to make BP-2, quenches this increase. A mechanism explaining these results is discussed. ...
3-Azido-..beta..-lactams react with the derivatives of trivalent phosphorus acids under mild conditions with the formation of 3-phosphoranediylamino-1,4-diaryl-2-azetidinones, which are readily hydrolyzed with the elimination of alcohol (thiol) to 3-phosphoranylamino-1,4-diaryl-2-azetidinones. The phosphine imide compounds obtained from the aryl alkyl phosphites are hydrolyzed with the elimination of phenols. 3-Phosphoranediylamino-1,4-diaryl-2-azetidinones react readily with alkyl and acyl halides with the formation of 3-(N-alkylphosphoryl-amino)- and 3-(N-acylphosphorylamino)-1,4-diaryl-2-azetidinones, respectively.
3-Azido-#beta#-lactams react with the derivatives of trivalent phosphorus acids under mild conditions with the formation of 3-phosphoranediylamino-1,4-diaryl-2-azetidinones, which are readily hydrolyzed with the elimination of alcohol (thiol) to 3-phosphoranylamino-1,4-diaryl-2-azetidinones. The phosphine imide compounds obtained from the aryl alkyl phosphites are hydrolyzed with the elimination of phenols. 3-Phosphoranediylamino-1,4-diaryl-2-azetidinones react readily with alkyl and acyl halides with the formation of 3-(N-alkylphosphoryl-amino)- and 3-(N-acylphosphorylamino)-1,4-diaryl-2-azetidinones, respectively.
Resistance to abrupt and gradual cold shock was determined in bioassays with pumpkinseed (Lepomis gibbosus), rainbow trout (Salmo gairdneri), and a northwestern crayfish (Pacifastacus leniusculus) acclimated to higher temperatures at 5 C increments. Test criteria were median tolerance limits (TLm) for 96-h exposures after abrupt cold shock, and 50 percent loss of equilibrium (LE50) for decline rates of 18, 15, 10, 5, and 1 C/h during gradual cold shock. Cold resistance depended on original acclimation temperature (AT) and varied among species under both test conditions in the order: pumpkinseed less than rainbow trout less than crayfish. The lower TLm limit for pumpkinseed was 12.3 C at 30 C AT, 9.6 C at 25 C AT, 4.5 C at 20 C AT, and 2.7 C at 15 C AT. Rainbow trout at 20, 15 and 10 C AT survived abrupt exposures to cold down to 3.3, 1.4 and 0.5 C, respectively. Crayfish at 25, 20 and 15 C AT survived exposures down to 2.5, 0.4 and 0.0 C, respectively. TLm values ...
Anthraquinones are widely present in plant kingdom, and clinically used as laxatives. Environmental contaminants, dioxins, develop various adverse effects through transformation of a cytosolic aryl hydrocarbon receptor (AhR). We investigated the effects of 18 anthraquinones and 7 of their structurally related compounds on transformation of the AhR estimated by its DNA-binding activity in the cell-free system. 1,4-Dihydroxyanthraquinone (quinizarin), 1,5-dihydroxyanthraquinone (anthrarufin), 1,8-dihydroxyanthraquinone (danthron), and 5-hydroxy-1,4-naphthoquinone (juglone) strongly suppressed DNA-binding activity of the AhR induced by 0.1 nM 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), with their IC(50) values around 1 muM. On the other hand, anthraquinone, 2,6-dihydroxyanthraquinone (anthraflavic acid), and 2-hydroxy-1,4-naphthalendione (lawsone) showed moderate effects. Quantitative structure-activity relationships analysis demonstrated that hydroxyl groups at C1 or ...
In addition to ceramics, alloys such as tool steel and nickel- and iron-based superalloys are being considered for high temperature applications such as missile bearings and low heat rejection engines. Studies were made to lubricate a nickel-based superalloy at 500{degrees}C, by using a vaporized aryl phosphate ester, at a concentration of 0.1% in air. From deposition and wear studies it was found that it was impossible to form a good polymeric coating on the superalloy surface. Energy dispersive X-ray analyzer (EDXA) analysis showed that this was due to minute quantities of aluminum in the alloy segregating to the surface, upon being heated to 500{degrees}C, forming a passive oxide coating. It was necessary to activate the surface, in order to lubricate the material successfully. A method of activation by electrodepositing the surface with a layer of iron oxide was developed. Once activated, a good lubricous polymer was formed on the superalloy surface. Tests ...
Ex situ and in situ fuel cell degradation of a sPAEK membrane were investigated. Post-mortem analyses of the aged membrane and of the degradation products eluted in water were carried out by NMR, IR, SEC and EDX. Ex situ agings were performed in a low concentration H{sub 2}O{sub 2} solution (0.07%) without any metallic catalyst. We exemplify that ex situ accelerated aging tests in such hydrogen peroxide solution are relevant to the chemical degradation in fuel cell. We have shown that a 500 h fuel cell test at moderate temperature (60 C) induces significant modifications on the macromolecules such as a 40% molecular weight reduction. Degradation appears heterogeneous and limited to the cathode side. The model compound approach developed in the previous article (Perrot et al.) has allowed the identification of the aging path in fuel cell. Phenolic and carboxylic acid chain ends have been identified as the main products resulting from polymer chain scissions. The ex situ lifetime (100 h) ...
Calcium-activated chloride channels (CaCCs) are widely expressed in mammalian tissues, including intestinal epithelia, where they facilitate fluid secretion. Potent, selective CaCC inhibitors have not been available. We established a high-throughput screen for identification of inhibitors of a human intestinal CaCC based on inhibition of ATP/carbachol-stimulated iodide influx in HT-29 cells after lentiviral infection with the yellow fluorescent halide-sensing protein YFP-H148Q/I152L. Screening of 50,000 diverse, drug-like compounds yielded six classes of putative CaCC inhibitors, two of which, 3-acyl-2-aminothiophenes and 5-aryl-2-aminothiazoles, inhibited by >95% iodide influx in HT-29 cells in response to multiple calcium-elevating agonists, including thapsigargin, without inhibition of calcium elevation, calcium-calmodulin kinase II activation, or cystic fibrosis transmembrane conductance regulator chloride channels. These compounds also inhibited ...
1-Furan-2-yl-3-pyridin-2-yl-propenone (FPP-3) is an anti-inflammatory agent with a propenone moiety and chemically synthesized recently. In this study, we examined the chemopreventive effect of FPP-3 on 7,12-dimethylbenz[a]anthracene (DMBA)-induced genotoxicity in MCF-7 cells. FPP-3 reduced the formation of the DMBA-DNA adduct. DMBA-induced CYP1A1 and CYP1B1 gene expression and enzyme activity were inhibited by FPP-3. It inhibited DMBA-induced aryl hydrocarbon receptor (AhR) transactivation and DMBA-inducible nuclear localization of the AhR. Induction of detoxifying phase II genes by chemopreventive agents represents a coordinated protective response against oxidative stress and neoplastic effects of carcinogens. Transcription factor NF-E2 related factor 2 (Nrf2) regulates antioxidant response element (ARE) of phase II detoxifying and antioxidant enzymes, such as glutathione S-transferase (GST) and NAD(P)H:quinone oxidoreductase (QR). FPP-3 increased the expression ...
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 ...