Bioorganic & Medicinal Chemistry Letters 2008-04-01

Fluorination of triptolide and its analogues and their cytotoxicity.

Yutaka Aoyagi, Yukio Hitotsuyanagi, Tomoyo Hasuda, Saki Matsuyama, Haruhiko Fukaya, Koichi Takeya, Ritsuo Aiyama, Takeshi Matsuzaki, Shusuke Hashimoto

Index: Bioorg. Med. Chem. Lett. 18(7) , 2459-63, (2008)

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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.