Abstract

SYNTHESIS AND CYTOTOXIC ACTIVITIES OF 3- BENZIMIDAZOLYL-CHALCONES DERIVATIVES

Aboudramane Kone, Mahama Ouattara, Doumade Zon, Anne-Caroline Chany, Sylvain Collet, Drissa Sissouma* and Ane Adjou

Abstract

The aim of this work was to synthesize new 3-benzimidazolylchalcones derivatives and to evaluate their anticancer activity and their cytotoxicity. We synthesized twelve chalcone derivatives by Claisen- Schmidt condensation method in basic medium and a chromenone by an iodine catalyzed cyclization reaction. The synthesized compounds were characterized by usual spectroscopic methods (1H and 13C NMR, MS).They were evaluated for their antitumor activity in vitro on the lung cancer cell line NCI-H727 but also for their cytotoxicity on a normal fibroblastic cell of human skin. These compounds have demonstrated good anticancer activities against human lung cancer cell with IC50 between 1.20 and 8.63 μM. They also showed a cytotoxicity on fibroblasts ranging from 0.61 to 9.29 μM. Futhermore, all these compounds were more effective than Rosco but less effective than Taxol used as references. Among these synthesized compounds, 4c and 4d were particularly advantageous with IC50 at 0.61 and 0.91 μM respectively.

Keywords: Benzimidazole, Chalcone, Chromenone, Lung cancer, Anticancer, Cytotoxicity.