Title of article
2,5-Diaminopyrimidines and 3,5-disubstituted azapurines as inhibitors of glycogen synthase kinase-3 (GSK-3)
Author/Authors
Christopher Lum، نويسنده , , Jeff Kahl، نويسنده , , Linda Kessler، نويسنده , , Jeff Kucharski، نويسنده , , Jan Lundstr?m، نويسنده , , Stephen Miller، نويسنده , , Hiroshi Nakanishi، نويسنده , , Yazhong Pei، نويسنده , , Kent Pryor، نويسنده , , Edward Roberts.، نويسنده , , Lubomir Sebo، نويسنده , , Robert Sullivan، نويسنده , , Jan Urban، نويسنده , , Zhijun Wang، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
4
From page
3578
To page
3581
Abstract
The discovery of two classes of pyrimidine-based inhibitors of GSK-3 is described. Optimization of these series led to inhibitors with IC50 < 10 nM and >100-fold selectivity over Aurora A kinase. A proposed binding mode of 21b is presented. One compound (33) of the pyrimidine series showed promising pharmacokinetic parameters.
Keywords
Diabetes , depression , Kinase inhibitors , GSK-3 , Aurora A , Molecular modeling , Alzheimer’s , bipolar disorder
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799604
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