Modular synthesis of radicicol a and related resorcylic acid lactones, potent kinase inhibitors

被引：70

作者：

Dakas, Pierre-Yves

Barluenga, Sofia

Totzke, Frank

Zirrgiebel, Ute

Winssinger, Nicolas

机构：

[1] Univ Strasbourg 1, Inst Sci & Ingn Supramol, CNRS, UMR 7006, F-67000 Strasbourg, France

[2] ProQinase GmbH, Freiburg, Germany

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2007年 / 46卷 / 36期

关键词：

inhibitors; resorcylic acid lactones; solid-phase extraction; total synthesis;

D O I：

10.1002/anie.200702406

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

(Chemical Equation Presented) Short and sweet: A concise and modular synthesis of radicicol A and related resorcylic acid lactones using fluorous isolation technology and immobilized reagents is reported (see scheme, R F = C3H6C6F13, TMSE = 2-(trimethylsilyl)-ethyl). The compounds are found to be potent (low-nanomolar) inhibitors of selected kinases. Despite their irreversible inactivation of kinases, they show good selectivity amongst a panel of 127 kinases. © 2007 Wiley-VCH Verlag GmbH & Co. KGaA.

引用

收藏

页码：6899 / 6902

页数：4

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