title: Thienyl and phenyl alpha-halomethyl ketones: new inhibitors of glycogen synthase kinase (GSK-3beta) from a library of compound searching.
abstract: Glycogen synthase kinase (GSK-3beta) plays a crucial role in Alzheimer's disease (AD). Its inhibition is a valid approach to the treatment of AD. In this initial letter, some thienyl and phenyl alpha-halomethyl ketones are described as new non-ATP competitive inhibitors of GSK-3beta. They are considered as lead compounds for designing and synthesizing new series, to carry out SAR studies, clear up the mechanism of action, and, in general, evaluate their therapeutical usefulness.
authors.affiliation: Instituto de Química Médica (CSIC), Juan de la Cierva 2, 28006 Madrid, Spain. SConde@iqm.csic.es
authors.forename: Santiago
authors.initials: S
authors.lastname: Conde
authors.forename: Daniel I
authors.initials: DI
authors.lastname: Pérez
authors.forename: Ana
authors.initials: A
authors.lastname: Martínez
authors.forename: Concepción
authors.initials: C
authors.lastname: Perez
authors.forename: Francisco J
authors.initials: FJ
authors.lastname: Moreno
mesh_terms: D000255:Adenosine Triphosphate / Q000737:chemistry; D016208:Databases, Factual; D038362:Glycogen Synthase Kinase 3 / Q000037:antagonists & inhibitors* / Q000737:chemistry; D000071679:Glycogen Synthase Kinase 3 beta; D007659:Ketones / Q000138:chemical synthesis* / Q000737:chemistry; D007700:Kinetics; D011485:Protein Binding; D013329:Structure-Activity Relationship
chemical_list: D007659:Ketones; D000255:Adenosine Triphosphate; D000071679:Glycogen Synthase Kinase 3 beta; D038362:Glycogen Synthase Kinase 3