Synthesis of Unsymmetrical C5-Curcuminoids as Potential Anticancer Agents

Abstract

Cancer and malaria are two major diseases, which have devastating effects on public health systems. In a quest of developing new anticancer and antimalarial agents, a series of 22 unsymmetrical C5-curcumionds was synthesized and evaluated for their anticancer activity against HeLa, KB, PC3 and DU145 cancer cell lines. Out of these, four compounds displayed potent activity in HeLa cancer cell line (IC50 ranging from 0.7 to 0.9 µM) than standard FDA-approved drug doxorubicin (IC50 = 1.7 µM). They also showed weak to moderate activity against other cancer cell lines. Unsymmetrical C5-curcumionids were also evaluated for their antimalarial activity against CQ-sensitive and CQ-resistant strains of P. falciparum. Weak antimalarial activities were observed with some compounds without any toxicity towards the mammalian cell line at the highest tested concentration of 10 µM. Keywords: Anticancer activity, Antimalarial activity, Curcumin, C5-curcuminoids, HeLa cancer cell line, Plasmodium falciparum.