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Thienyl and Phenyl α-Halomethyl Ketones:  New Inhibitors of Glycogen Synthase Kinase (GSK-3β) from a Library of Compound Searching

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journal contribution
posted on 20.09.2003, 00:00 by Santiago Conde, Daniel I. Pérez, Ana Martínez, Concepción Perez, Francisco J. Moreno
Glycogen synthase kinase (GSK-3β) 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 α-halomethyl ketones are described as new non-ATP competitive inhibitors of GSK-3β. 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 therapheutical usefulness.