The Bhas 42 cell transformation assay is a short-term system using a clone of the BALB/c 3T3 cells transfected with an oncogenic murine ras gene (v-Ha-ras). The assay has previously been reported to be capable of detecting the tumor-initiating and tumor-promoting activities of chemical carcinoge...
Sodium dodecyl sulfate (SDS)-induced coagulation of poly(allylamine hydrochloride) [PAH] was studied for the rapid removal of estrogens and phenolic compounds from water. When electrically equivalent amount (62 mg L−1) of SDS was added into the aqueous solution of 20 mg L−1 PAH with vigorous mix...
Various additives viz. hydrotropes, bile salts, fatty acid and cyclodextrin effect on the cloud point (CP) behavior of amphiphilic drug promazine hydrochloride (PMZ) in 1 mmol dm−3 14-4-14 + 10 mmol dm−3 sodium phosphate (SP) buffer solutions have been investigated in the present study. These va...
In the present study, a series of 4-(1-aryl-5-chloro-2-oxo-1,2-dihydro-indol-3-ylideneamino)-N-substituted benzene sulfonamides (1–20) was synthesized and screened for their in vitro antimicrobial activity against Gram positive, Gram negative bacterial and fungal strains indicating that compoun...
Optimization of benzoic acid derivatives by introducing substituents into the diphenyl urea moiety led to the identification of compound 20l as a potent VLA-4 antagonist. Compound 20l inhibited eosinophil infiltration into bronchial alveolar lavage fluid in a murine asthma model by oral dosing a...
3-Naphthyl-1-phenyl-5-(5-fluoro-2-nitrophenyl)-2-pyrazoline (NPFP), a fluorogenic probe and its derivative NPFP-Phenylephrine were synthesized and their absorption and fluorescence properties were recorded in solvents of varying polarity. Spectroscopic studies reveal that, the solvatochromic beh...
A common strategy to synthesize 4/6-(4-(4-methylpiperazin-1-yl)-6-(4-(4-oxo-2-phenylthiazolidin-3-yl)phenyl)-1,3,5-triazin-2-yloxy)benzonitriles/nicotinonitriles was developed by applying an efficient palladium-catalyzed C–C Suzuki coupling. Moreover, the synthesized compounds were also tested ...
Estrogen receptor (ER) antagonist, tamoxifen has been universally used for the treatment of the ER-positive breast cancer; however, the inevitable emergence of resistance to tamoxifen obstructs the successful treatment of this cancer. So, there is an immediate requirement for the search of a nov...
An interface bioreactor, which is a device for the microbial transformation of water-insoluble substrates, was applied to an anaerobic bioconversion for the first time. Methyl 7-ketolithocholate [Me-7KLCA] was reduced with the human intestinal bacterium Eubacterium aerofaciens JCM 7790 in a conv...
Because ursodeoxycholic and chenodeoxycholic acids are interconverted in humans via 7-ketolithocholic acid, bile acid metabolism was studied in the nutria (Myocastor coypus), the bile of which is known to contain these three bile acids. Relative concentrations of ursodeoxycholic (37% ± 20%), 7-...
Ferulic acid (4-hydroxy-3-methoxycinnamic acid; FA) is a plant constituent and is contained in several medicinal plants for clinical use. In this paper, we investigated the effects of FA on the proliferation of neural stem/progenitor cells (NSC/NPCs) in vitro and in vivo. FA significantly increa...
Esters, acyloximes, amides and acid anhydrides have been prepared from the respective carboxylic acids, oximes, amines and alcohols by the use of the reagent combination BrCCl3-PPh3. The reactions obviate the handling acyl halides or more aggressive reagents PCl3, POCl3, or SOCl2. Furthermore, t...
To explore novel high efficiency and low toxicity antitumor agents, a series of dihydroartemisinin-cinnamic acid ester derivatives modified on C-12 and/or C-9 position (s) were synthesized and the in vitro antitumor activities against PC-3, SGC-7901, A549 and MDA-MB-435s cancer cell lines were a...
Chlorogenic acid lactones have been identified as key contributors to coffee bitterness. These compounds are formed during roasting by dehydration and cyclization of their precursors, the chlorogenic acids (CGAs). In the present study, we investigated an approach to decompose these lactones in a...
4-Hydroxy benzaldehyde dehydrogenase catalyses a step in a well-studied pathway for the catabolism of 4-hydroxy-substituted cinnamates in Acinetobacter baylyi, oxidising a benzaldehyde group to the corresponding benzoic acid, with the concomitant reduction of NAD+ to NADH. Although much genetic ...
Optically transparent crystal of the organic salt DEASI (2-[2-(4-Diethylamino-phenyl)-vinyl]-1-methyl-pyridinium iodide) has been synthesized by using knoevenagel condensation reaction method. The synthesized material has been purified by successfully recrystallization process. Single crystals o...
Reaction of bis(4-hydrazinylphenyl)methane with 4-substitutedbenzaldehyde in the presence of CH3COONa in EtOH at 80 °C yields bis(4-((E)-2-(4-substitutedbenzylidene)hydrazinyl)phenyl) methane [−N(CH3)2 1, −F 2, −Cl 3, −NO2 4], which subsequently in the presence of CCl4, CuCl and tetramethylethy...
Mitochondrial dynamics are associated with the development of porcine embryos. However, little is known about the effects of mitochondrial dynamics-related genes (Drp1 and pDrp1-Ser616) on early porcine embryo development. Here, we investigated the effect of Drp1-dependent mitochondrial fission ...
Here we have presented a sensitive and selective LC-MS/MS method for the quantification of tyrphostin A9, which is a selective inhibitor for platelet derived growth factor receptor tyrosine kinase and has been investigated in vitro as a potent oxidative phosphorylation uncoupler. The murine anal...
2-Phenyl-4-quinolone and 9-oxo-9,10-dihydroacridine derivatives were synthesized and screened as potential antitumor promoters by examining the ability of the compounds to inhibit Epstein–Barr virus early antigen (EBV-EA) activation induced by the tumor promoter 12-O-tetradecanoylphorbol-13-ace...
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