Rational design of potent GSK3beta inhibitors with selectivity for Cdk1 and Cdk2
Dominique Lesuisse1, Gilles Dutruc-Rosset, Gilles Tiraboschi
1Medicinal Chemistry, 13 Quai Jules Guesde, 94300 Vitry-sur-Seine, France. dominique.lesuisse@sanofi-aventis.com
Bioorganic & Medicinal Chemistry Letters
|February 20, 2010
Abstract:
From an HTS hit, a series of potent and selective inhibitors of GSK3beta have been designed based on a Cdk2-homology model and with the help of several crystal structures of the compounds within Cdk2.
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