Thienyl and phenyl alpha-halomethyl ketones: new inhibitors of glycogen synthase kinase (GSK-3beta) from a library of compound searching.
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.
Conde
Santiago
S
Instituto de Química Médica (CSIC), Juan de la Cierva 2, 28006 Madrid, Spain. SConde@iqm.csic.es
Pérez
Daniel I
DI
Martínez
Ana
A
Perez
Concepción
C
Moreno
Francisco J
FJ
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
D007659:Ketones; D000255:Adenosine Triphosphate; D000071679:Glycogen Synthase Kinase 3 beta; D038362:Glycogen Synthase Kinase 3