Synthesis and antiangiogenic activity of thioacetal artemisinin derivatives.
Various thioacetal artemisinin derivatives can inhibit the angiogenesis and might be angiogenesis inhibitors. In particular, 10 alpha-phenylthiodihydroartemisinins (5), 10 beta-benzenesulfonyl-9-epi-dihydroartemisinin (11) and 10 alpha-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 microg/egg by 90%.
Oh
Sangtae
S
Department of Chemistry, Yonsei University, Wonju 220-710, South Korea.
Jeong
In Howa
IH
Ahn
Chan Mug
CM
Shin
Woon-Seob
WS
Lee
Seokjoon
S
D000080:Acetals / Q000737:chemistry*; D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D037621:Artemisinins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D002642:Chick Embryo; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects; D008401:Gas Chromatography-Mass Spectrometry; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D012717:Sesquiterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared
D000080:Acetals; D020533:Angiogenesis Inhibitors; D037621:Artemisinins; D012717:Sesquiterpenes; C031327:artemisinin