C-Glycosylated cinnamoylfuran derivatives as novel anti-cancer agents

Abstract

A series of C-glycosylated cinnamoylfuran derivatives were synthesized in excellent yield from free sugars. The C-glycosylated furan derivatives were prepared under aqueous reaction conditions. The anticancer potentials of the synthesized compounds were evaluated on the basis of their comparative cytotoxic effects on cancer cells (MCF-7 and HeLa) and normal cells (NKE). Among 28 compounds evaluated for their cytotoxic effects on cancer cells, three compounds (compounds 8, 24 and 28) were shown to have significant cytotoxic effects on MCF-7 and HeLa cell lines and comparatively less toxicity against normal NKE cell line. Based on its selectivity index, compound 24 was considered the most promising anticancer agent amongst the above three compounds. Further biochemical studies with compound 24 showed that both intrinsic and extrinsic pathways of apoptosis contribute to compound 24 mediated cytotoxicity.