Fluorination of triptolide and its analogues and their cytotoxicity

被引：40

作者：

Aoyagi, Yutaka ^{[1
]}

Hitotsuyanagi, Yukio ^{[1
]}

Hasuda, Tomoyo ^{[1
]}

Matsuyama, Saki ^{[1
]}

Fukaya, Haruhiko ^{[1
]}

Takeya, Koichi ^{[1
]}

Aiyama, Ritsuo ^{[2
]}

Matsuzaki, Takeshi ^{[2
]}

Hashimoto, Shusuke ^{[2
]}

机构：

[1] Tokyo Univ Pharm & Life Sci, Sch Pharm, Tokyo 1920392, Japan

[2] Yakult Cent Inst Microbiol Res, Tokyo 1868650, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 07期

关键词：

triptolide; semisynthesis; cytotoxicity; SAR; fluorination; Tripterygium wilfordii;

D O I：

10.1016/j.bmcl.2008.02.039

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

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, 14 beta-dehydroxy-14 beta-fluoro triptolide, was found to be more cytotoxic than the parent natural triptolide. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：2459 / 2463

页数：5

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