New 3-[(4-Hydroxy-6-Methly-2(1H)-Pyridinones)-3-yl]-4-Substituted-(1H)-1,2,4-Triazole-5-Thiones: Efficient Synthesis, X-Ray Crystallographic Analysis, and Antitumor Activity

Abstract

Fifteen new 3-[(4-hydroxy-6-methly-2(1H)-pyridinones)-3-yl]-4-substituted- (1H)-1,2,4-triazole-5- thione compounds were synthesized from methyl 4-hydroxy-6- methyl-2-oxo-1,2-dihydropyridine-3- carboxylate in good overall yields by four step reactions. Molecular structure of these compounds was confirmed by IR, NMR, MS, elemental analysis and X-ray diffraction. Their antitumor activities were evaluated in vitro by the SRB and MTT methods. The results show that there are two compounds which are highly effective against KB cells and one compound which is highly effective against Bel-7402 cells. Keywords: 1,2,4-triazole, antitumor activity, Schiff base, hydroxypyridin-2(1H)-one, biological activity, potential antitumor medicine