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Fluorination of triptolide and its analogues and their cytotoxicity
Authors:Aoyagi Yutaka  Hitotsuyanagi Yukio  Hasuda Tomoyo  Matsuyama Saki  Fukaya Haruhiko  Takeya Koichi  Aiyama Ritsuo  Matsuzaki Takeshi  Hashimoto Shusuke
Affiliation:School of Pharmacy, Tokyo University of Pharmacy & Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.
Abstract:The reaction of triptolide and its analogues with a fluorinating agent, that is, bis(2-methoxyethyl)aminosulfur trifluoride (Deoxo-Fluor) or (diethylamino)sulfur trifluoride (DAST), was studied. One of the fluorinated products, 14beta-dehydroxy-14beta-fluoro triptolide, was found to be more cytotoxic than the parent natural triptolide.
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