Cytotoxic Activity of Some New Azole derivatives

Abstract

Azole derivatives are an important class of compounds in medicinal chemistry with a wide variety of biological activities. We previously described synthesis and antimicrobial evaluations of some new Azole derivatives. Most of our compounds showed desirable activity against different species of microorganisms. Here, we chose seventeen of these compounds, in four different groups including imidazole (group a, 1a-6a), 2-methylimidazole (group b, 1b-4b), 2-methyl-4-nitroimidazole (group c, 1c-4c) and benzimidazole (group d, 1d-3d) to further evaluate their cytotoxic activities against a human cancer cell line (HepG2) using colorimetric MTT cytotoxic assay. We also compared their cytotoxic activities with Clotrimazole to find the safer compounds as antimicrobial agents. Our results indicated that Azole compounds including 2b, 4c, 2d and 3d displayed desirable anti-tumor activities against HepG2 (IC50<50µM) and might be considered as potential anticancer agents for further studies. We also showed that most of our synthesized compounds had less cytotoxicity compared to Clotrimazole which could introduce them as good candidates for antimicrobial agents. Keywords: Azole, Anti-tumor activity, MTT, HepG2