Abstract

SYNTHESIS, CHARACTERIZATION, MOLECULAR DOCKING OF SOME NOVEL BENZOFURAN CHALCONE DERIVATIVES AND THEIR EVALUATION OF INVITRO ANTI CANCER ACTIVITY

*Kathiravan M., Umarani G. and Abdul Hassan Sathali

Abstract

A series of Novel benzofuran chalcone derivatives have been synthesised in multiple steps with the suitable claisen schmidt condensation reaction procedures and then well characterized by various analytical techniques. All the synthesised compounds were evaluated for their invitro anticancer activity against two human cell lines includes Human breast cancer cells (MCF-7) and human liver cell lines (HepG2) at various concentrations. The results were shown in terms of percentage cell viability reduction and IC50 values. Amoung all the five synthsesied compounds, Compounds 5a and 5b has showed potent activity against breast cancer cells (MCF-7) And the synthesised compounds 5c and 5d has showed significant activity against Liver cells (HepG2). Furthermore, the structure and anticancer activity relationship was supported by molecular docking study of the major potent compounds 5a, 5b and 5c.The compounds 5a, 5b and 5c were dock against the two major target proteins. The PDB id of 1MOX (lung cancer) and 2DSQ (breast epithelian cancer) were selected and obtained from protein data bank (PDB) selected for INSILICO study and the protein-ligand binding site was analysed and visualized. Its results majorly compounds 5a and 5b are the best binding pose with targets.

Keywords: Benzofuran chalcone derivatives, Claisen schmidt condensation reaction, Invitro- anticancer activity, Insilico molecular docking study.