Synthesis and antiangiogenic activity of thioacetal artemisinin derivatives Original Research Article

Various thioacetal artemisinin derivatives can inhibit the angiogenesis and might be angiogenesis inhibitors. In particular, 10α-phenylthiodihydroartemisinins (5), 10β-benzenesulfonyl-9-epi-dihydroartemisinin (11) and 10α-mercaptodihydroartemisinin (13) exhibit strong growth inhibition activity against HUVEC proliferation. Compound 11 have a good inhibitiory activity upon HUVEC tube formation, and 5 and 11 show a strong inhibitory effect on angiogenesis using CAM assay at 5 μg/egg by 90%.