Yang Rui
2008
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Journal
Chinese Journal of Applied Chemistry
Abstract
To discover a novel structural lead compound for developing antitumor agents, 4-amino-5-pyridin-3-yl-1,2,4-triazole-3-thiol(1) was S-etherized with iodomethane to give the intermediate of 4-amino-3-methylsulfanyl-5-pyridin-3-yl-1,2,4-triazole(2) followed by condensation with various aromatic aldehydes to afford the title compounds of seven novel Schiff bases, 4-(aromatic methyl)imino-3-methylsulfanyl-5-pyridin-3-yl-1,2,4-triazoles(3a~3g). Their antitumor activity against SMMC-7721 and Bel-7402 cells were evaluated by MTT method in vitro, and their structures were characterized by IR, 1H NMR, MS spectrum data and elemental analysis. Among synthesized compounds, 3c, 3e and 3f showed potential antitumor activity with the IC50 of 3.8, 2.0,1.3 and 2.5, 2.5, 1.1 μmol/L against SMMC-7721 and Bel-7402 cells, respectively.