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Huang Y.,Bengbu Medical College | Huang Y.,Research and Development Center for Fine Chemicals | Liu F.,Bengbu Medical College | Zhao L.,Bengbu Medical College | And 2 more authors.
Cell Biology International | Year: 2012

In order to create novel, potent and selective anti-cancer agents, the action of 4-(4-fluorophenyl)amino-5,6,7-trimethoxyquinazoline (compound 1018) on 10 different kinds of tumour cells were assayed by MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide]. It possesses a broad spectrum of anti-cancer activity. The mechanism of action of 4-(4-fluorophenyl)amino-5,6,7-trimethoxyquinazoline (hereafter referred to as compound 1018) against tumour cells was studied in androgen-independent prostate cancer PC-3 cells by microscopic observation, LDH (lactate dehydrogenase) release assay and Western blotting. Its activity was dose-dependent, with an IC 50 of 13.0±1.4 μM after 72 h treatment. Microscopy and LDH release assay indicated that the effect was through anti-proliferation rather than cytotoxicity. Western blot analysis also showed that treatment of cells with 50 mM compound 1018 for 30 min almost completely inhibited EGF (epidermal growth factor)-induced phosphorylation of ERK1/2 (extracellular-signal-regulated kinase 1/2), which suggests that its anti-proliferative effect is largely associated due to ERK1/2 activation being inhibited. Thus compound 1018 is a potential anti-cancer agent. © The Author(s) Journal compilation © 2012 Portland Press Limited. Source

Yang C.,Research and Development Center for Fine Chemicals | Yang S.,Research and Development Center for Fine Chemicals | Song B.,Research and Development Center for Fine Chemicals | Hu D.,Research and Development Center for Fine Chemicals | And 6 more authors.
Chinese Journal of Organic Chemistry | Year: 2010

Starting from p-nitrobenzoic acid and p-methoxybenzoic acid, seven new 2-sub-stitutedthio-5-(4-nitro or 4-methoxyphenyl)-1,3,4-thiadiazole compounds 5 were synthesized in five steps including esterification, hydrazidation, salt formation, cyclization and thioetherification. Treatment of 5 with H 2O2 catalyzed by ammonium molybdate in ethanol afforded the ten 2-substituted sulfonyl-5-(4-nitro or 4-methoxyphenyl)1,3,4-thiadiazole 6 with good yields. The structures of the new compounds synthesized were confirmed by 1H NMR, 13C NMR, IR spectra and elemental analysis. The preliminary bioassay showed that compound 5d had good antifungal activity against Fusarium graminearum, Fusarium oxysporum and Cytospora mandshurica with the rate of 99.0%, 100.0% and 100.0% at the concentration of 500 μg·mL-1, and compound 6j possessed high inhibitory effect with rate of 47.7%, 46.4% and 50.6% at the concentration of 50 μg·mL-1. Source

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