1-azakenpaullone is a selective inhibitor of glycogen synthase kinase-3β

被引：158

作者：

Kunick, C

Lauenroth, K

Leost, M

Meijer, L

Lemcke, T

机构：

[1] Tech Univ Carolo Wilhelmina Braunschweig, Inst Pharmazeut Chem, D-38106 Braunschweig, Germany

[2] Univ Hamburg, Inst Pharm, Abt Pharmazeut Chem, D-20146 Hamburg, Germany

[3] CNRS, Biol Stn, F-29682 Roscoff, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 02期

关键词：

D O I：

10.1016/j.bmcl.2003.10.062

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Kenpaullone derivatives with a modified parent ring system were synthesized in order to develop kinase inhibitors with enhanced selectivity. Among the novel structures, 1-azakenpaullone was found to act as a selective GSK-3beta versus CDK1 inhibitor. The charge distribution within the 1-azakenpaullone molecule is discussed as a possible explanation for the enhanced GSK-3beta selectivity of 1-azakenpaullone compared to other paullone derivatives. (C) 2003 Elsevier Ltd. All rights reserved.

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页码：413 / 416

页数：4

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