Novel GSK-3 inhibitors with improved cellular activity

…, JA Boucheron, SL Schweiker, SH Dickerson…

Index: Peat, Andrew J.; Garrido, Dulce; Boucheron, Joyce A.; Schweiker, Stephanie L.; Dickerson, Scott H.; Wilson, Jayme R.; Wang, Tony Y.; Thomson, Stephen A. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 9 p. 2127 - 2130

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Citation Number: 41

Abstract

A novel series of [1-(1H-benzimidazol-7-yl)-1H-pyrazolo [3, 4-d] pyrimidin-4-yl] arylhydrazones was synthesized and shown to potently inhibit glycogen synthase kinase-3 (GSK-3). In light of detailed structure–activity relationships and structural knowledge of the GSK-3 binding pocket, a benzimidazole substituent was incorporated onto the pyrazolopyrimidine core resulting in improved potency over previous analogs. More ...