Divergent synthesis of a pochonin library targeting HSP90 and in vivo efficacy of an identified inhibitor

被引：48

作者：

Barluenga, Sofia ^{[1
]}

Wang, Cuihua ^{[1
]}

Fontaine, Jean-Gonzague ^{[1
]}

Aouadi, Kaiss ^{[1
]}

Beebe, Kristin ^{[2
]}

Tsutsumi, Shinji ^{[2
]}

Neckers, Len ^{[2
]}

Winssinger, Nicolas ^{[1
]}

机构：

[1] Univ Strasbourg 1, Inst Sci & Ingn Supramol, F-67000 Strasbourg, France

[2] NCI, Urol Oncol Branch, Bethesda, MD 20892 USA

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2008年 / 47卷 / 23期

关键词：

antitumor agents; bioorganic chemistry; natural products; solid-phase synthesis; synthesis design;

D O I：

10.1002/anie.200800233

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

(Chemical Equation Presented) Make a clean breast of it: The generation of a library of pochonin Dderivatives by a solid-phase approach has led to the discovery of pochoxime (see scheme), a potent inhibitor of the heat-shock protein 90, with over 100-fold improved incellular activity. Pochoxime was found to be effective in breast tumor xenografts, leading to a reduction in the tumor size. © 2008 Wiley-VCH Verlag GmbH & Co. KGaA.

引用

页码：4432 / 4435

页数：4

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