Synthesis and antiangiogenic activity of thioacetal artemisinin derivatives

Various thioacetal artemisinin derivatives can inhibit the angiogenesis and might be angiogenesis inhibitors. In particular, 10alpha-phenylthiodihydroartemisinins (5), 10beta-benzenesulfonyl-9-epi-dihydroartemisinin (14) and 10alpha-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 mug/egg by 90%. (C) 2004 Elsevier Ltd. All rights reserved.