title: Rational design of potent GSK3beta inhibitors with selectivity for Cdk1 and Cdk2.
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.
authors.affiliation: Medicinal Chemistry, 13 Quai Jules Guesde, 94300 Vitry-sur-Seine, France. dominique.lesuisse@sanofi-aventis.com
authors.forename: Dominique
authors.initials: D
authors.lastname: Lesuisse
authors.forename: Gilles
authors.initials: G
authors.lastname: Dutruc-Rosset
authors.forename: Gilles
authors.initials: G
authors.lastname: Tiraboschi
authors.forename: Matthias K
authors.initials: MK
authors.lastname: Dreyer
authors.forename: Sébastien
authors.initials: S
authors.lastname: Maignan
authors.forename: Alain
authors.initials: A
authors.lastname: Chevalier
authors.forename: Frank
authors.initials: F
authors.lastname: Halley
authors.forename: Philippe
authors.initials: P
authors.lastname: Bertrand
authors.forename: Marie-Claude
authors.initials: MC
authors.lastname: Burgevin
authors.forename: Dominique
authors.initials: D
authors.lastname: Quarteronet
authors.forename: Thomas
authors.initials: T
authors.lastname: Rooney
mesh_terms: D016203:CDC2 Protein Kinase / Q000037:antagonists & inhibitors*; D051357:Cyclin-Dependent Kinase 2 / Q000037:antagonists & inhibitors*; D015195:Drug Design; D038362:Glycogen Synthase Kinase 3 / Q000037:antagonists & inhibitors*; D000071679:Glycogen Synthase Kinase 3 beta; D008958:Models, Molecular; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D013379:Substrate Specificity
chemical_list: D047428:Protein Kinase Inhibitors; D000071679:Glycogen Synthase Kinase 3 beta; D016203:CDC2 Protein Kinase; D051357:Cyclin-Dependent Kinase 2; D038362:Glycogen Synthase Kinase 3