Identification of 2-(4-pyridyl) thienopyridinones as GSK-3β inhibitors

…, A Pozzan, G Merlo, P Marzorati, P Bamborough…

Index: Gentile, Gabriella; Bernasconi, Giovanni; Pozzan, Alfonso; Merlo, Giancarlo; Marzorati, Paola; Bamborough, Paul; Bax, Benjamin; Bridges, Angela; Brough, Caroline; Carter, Paul; Cutler, Geoffrey; Neu, Margarete; Takada, Mia Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 16 p. 4823 - 4827

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Citation Number: 15

Abstract

The discovery of a novel series of 2-(4-pyridyl) thienopyridinone GSK-3β inhibitors is reported. X-ray crystallography reveals its binding mode and enables rationalization of the SAR. The initial optimization of the template for improved cellular activity and predicted CNS penetration is also presented.