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
收藏
页码：1985 / 1989
页数：5
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