Synthesis of a novel series of highly functionalized Baylis–Hillman adducts of artemisinin with potent anticancer activity

A novel series of densely functionalized derivatives of artemisinin have been synthesized using Baylis–Hillman reaction and their further applicability has been demonstrated. The in vitro anticancer activity of these adducts against a panel of human cancer cell lines is summarized. Compound 10 (% GI of 100 against colon colo-205; % GI of 85 against Lung A-549), 7b (% GI of 78 against prostrate PC-3) and 9a, 9b (% GI of 71 against prostrate PC-3) were especially potent in inhibiting the growth of certain human cancer cell lines and were comparable to that of clinically used anticancer drugs. These newly synthesized compounds can be further utilized as potential precursor for the synthesis of libraries of new artemisinin analogs including dimer.