title: 6-heteroaryl-pyrazolo[3,4-b]pyridines: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3).
abstract: A series of 6-heteroaryl-pyrazolo[3,4-b]pyridines has been optimised to afford potent inhibitors of Glycogen Synthase Kinase-3 (GSK-3). These analogues display excellent selectivity over the closely related Cyclin Dependent Kinase-2 (CDK-2).
authors.affiliation: Department of Medicinal Chemistry, Neurology & GI Centre of Excellence for Drug Discovery, GlaxoSmithKline Research Limited, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. jason_witherington@gsk.com
authors.forename: Jason
authors.initials: J
authors.lastname: Witherington
authors.forename: Vincent
authors.initials: V
authors.lastname: Bordas
authors.forename: Alessandra
authors.initials: A
authors.lastname: Gaiba
authors.forename: Antoinette
authors.initials: A
authors.lastname: Naylor
authors.forename: Anthony D
authors.initials: AD
authors.lastname: Rawlings
authors.forename: Brian P
authors.initials: BP
authors.lastname: Slingsby
authors.forename: David G
authors.initials: DG
authors.lastname: Smith
authors.forename: Andrew K
authors.initials: AK
authors.lastname: Takle
authors.forename: Robert W
authors.initials: RW
authors.lastname: Ward
mesh_terms: D000818:Animals; D042846:CDC2-CDC28 Kinases / Q000037:antagonists & inhibitors; D051357:Cyclin-Dependent Kinase 2; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D038362:Glycogen Synthase Kinase 3 / Q000037:antagonists & inhibitors*; D006801:Humans; D006860:Hydrogen Bonding; D020128:Inhibitory Concentration 50; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D011725:Pyridines; D042846:CDC2-CDC28 Kinases; C495894:CDK2 protein, human; D051357:Cyclin-Dependent Kinase 2; D038362:Glycogen Synthase Kinase 3