Rational design of potent GSK3β inhibitors with selectivity for Cdk1 and Cdk2

被引：24

作者：

Lesuisse, Dominique ^{[1
,5
]}

Dutruc-Rosset, Gilles ^{[1
,5
]}

Tiraboschi, Gilles ^{[3
,5
]}

Dreyer, Matthias K. ^{[6
]}

Maignan, Sebastien ^{[4
,5
]}

Chevalier, Alain ^{[1
,5
]}

Halley, Frank ^{[1
,5
]}

Bertrand, Philippe ^{[2
,5
]}

Burgevin, Marie-Claude ^{[2
,5
]}

Quarteronet, Dominique ^{[2
,5
]}

Rooney, Thomas ^{[2
,5
]}

机构：

[1] Med Chem, F-94300 Vitry Sur Seine, France

[2] CNS Dept, F-94300 Vitry Sur Seine, France

[3] CAS Mol Modelling, F-94300 Vitry Sur Seine, France

[4] CAS Struct Biol, F-94300 Vitry Sur Seine, France

[5] Sanofi Aventis, F-94300 Vitry Sur Seine, France

[6] Sanofi Aventis, D-65926 Frankfurt, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 06期

关键词：

Glycogen synthase kinase; GSK3; beta; Aminoindazole; Cdk's; SYNTHASE KINASE-3 GSK-3; CRYSTAL-STRUCTURE; PROTEIN;

D O I：

10.1016/j.bmcl.2010.01.114

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

From an HTS hit, a series of potent and selective inhibitors of GSK3 beta have been designed based on a Cdk2-homology model and with the help of several crystal structures of the compounds within Cdk2. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：1985 / 1989

页数：5

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