Synthesis and anticancer activity evaluation of resveratrol–chalcone conjugates

Abstract

A series of novel resveratrol–chalcone conjugates have been synthesized. Four compounds were evaluated for their anticancer activity against 60 human cancer cell lines. Among all the derivatives, compound 70 was found to be the most active and showed high selectivity towards certain ovarian cancer, non-small cell lung cancer and breast cancer cell lines with GI50 values in the range of 1.28–34.1 μM. Docking studies were performed to determine the probable binding mode of these compounds in the colchicine–tubulin binding site. A strong H-bonding interaction (1.852 Å) was observed with Cys-241 amino acid present in the binding pocket. Thus we believe that compound 70 may possibly be used as a lead for the development of new anticancer agents.