Synthesis and evaluation of cardamonin derivatives as antiproliferative agents to human cancer cells

Twenty novel cardamonin derivatives were synthesized and evaluated for antiproliferative activity against four cancer cell lines (HT-29, DLD-1, MDA-MB-231, and HepG2). Among the derivatives, SWA2 showed the most potent effects with an IC50 value of 4.43-11.0 mu M against three cancer cell lines except for HepG2. Further investigation showed that SWA2 induced cancer cell death by apoptosis. Flow cytometry analysis showed that SWA2 treatment increased the ratio of apoptotic and dead cells. Further western blot analysis revealed that SWA2 treatment increased cleaved PARP. In summary, SWA2 can be utilized as a lead structure for anticancer therapy.