Enhanced potency of perfluorinated thalidomide derivatives for inhibition of LPS-induced tumor necrosis factor-α production is associated with a change of mechanism of action

被引：19

作者：

Niwayama, S

Loh, C

Turk, BE

Liu, JO ^{[1
]}

Miyachi, H

Hashimoto, Y

机构：

[1] MIT, Ctr Canc Res, Cambridge, MA 02139 USA

[2] MIT, Dept Biol, Cambridge, MA 02139 USA

[3] MIT, Dept Chem, Cambridge, MA 02139 USA

[4] Univ Tokyo, Inst Mol & Cellular Biosci, Bunkyo Ku, Tokyo 113, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(98)00171-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Perfluorination of phthalimides leads to dramatically increased potency as inhibitors of TNF-alpha production. We examined the enantiodependence for several tetrafluorophthalimides and alpha-methylthalidomide, 3. Only 3 exhibited strikingly enantiodependent activity. The key structural determinant for the enhanced activity is the tetrafluorophthaloyl group, which confers enhanced potency and a change in the mechanism of inhibition. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：1071 / 1076

页数：6

共 21 条

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