Design, synthesis and biological evaluation of imidazopyridine/pyrimidine-chalcone derivatives as potential anticancer agents

A new series of imidazo[2,1-b]pyridine/pyrimidine chalcone derivatives were synthesized and evaluated for their anticancer activity. These chalcone derivatives showed promising activity with GI(50) values ranging from 0.28 to 30.0 mu M. The detailed biological aspects of one of the promising compound 31 on the MCF-7 cell line were studied. Interestingly, compound 3f induced GI cell cycle arrest, down regulation of GI phase cell cycle regulatory proteins such as cyclin DI, El, and CDK2. Moreover, compound 31 showed the characteristic features of apoptosis such as enhancement in the levels of p27 and TNFRI proteins with concomitant down regulation of procaspase-9. One of the representative compound of this series 3f could be considered as the potential lead for its development as a new anticancer agent.