Synthesis and biological evaluation of 3-amino-1,2,4-triazole derivatives as potential anticancer compounds

Abstract

Two series of compounds carrying 3-amino-1,2,4-triazole scaffold were synthesized and evaluated for their anticancer activity against a panel of cancer cell lines using XTT assay. The 1,2,4-triazole synthesis was revisited for the first series of pyridyl derivatives. The biological results revealed the efficiency of the 3-amino-1,2,4-triazole core that could not be replaced and a clear beneficial effect of a 3-bromophenylamino moiety in position 3 of the triazole for both series (compounds 2.6 and 4.6) on several cell lines tested. Moreover, our results point out an antiangiogenic activity of these compounds. Overall, the 5-aryl-3-phenylamino-1,2,4-triazole structure has promising dual anticancer activity.

Keywords: 1, 2, 4-Triazole; 3-Amino-1, 2, 4-triazole; 5-Pyridotriazole; Anti-angiogenesis drug; Anticancer agent.