Anti-tumor activity of new artemisinin-chalcone hybrids

In an attempt to develop potent and selective anti-tumor agents, three new series of artemisinin-chalcone hybrids 10a-10g, 11a-11g and 12a-12h were designed, synthesized and screened for their anti-tumor activity against five cell lines (HT-29, A549, MDA-MB-231, HeLa and H460) in vitro. Among compounds 10a-g and 11a-11g, most of them displayed enhanced activity and good selectivity toward HT-29 and HeLa cell lines with IC(50) values ranging from 0.12 to 0.85 µM as compared with DHA (dihydroartemisinin). Compounds 10a and 11a are most active toward HeLa cells with IC(50) values of 0.12 and 0.19 µM. The results revealed that the presence of chalcone moiety is beneficial to their activity and selectivity. In addition, compounds 12a-12h containing a 'reversed chalcone' moiety showed only slight improvement in activity than those of DHA.