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

Authors :
Gilles Dutruc-Rosset
Sébastien Maignan
Alain Chevalier
Frank Halley
Thomas Rooney
Matthias K. Dreyer
Dominique Lesuisse
Gilles Tiraboschi
Dominique Quarteronet
Philippe Bertrand
Marie-Claude Burgevin
Source :
Bioorganic & Medicinal Chemistry Letters. 20:1985-1989
Publication Year :
2010
Publisher :
Elsevier BV, 2010.

Abstract

From an HTS hit, a series of potent and selective inhibitors of GSK3β have been designed based on a Cdk2-homology model and with the help of several crystal structures of the compounds within Cdk2.

Details

ISSN :
0960894X
Volume :
20
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry Letters
Accession number :
edsair.doi.dedup.....52fd7bd1858589017041fe68fdcfe9e7
Full Text :
https://doi.org/10.1016/j.bmcl.2010.01.114