1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3β

…, K Lauenroth, M Leost, L Meijer, T Lemcke

Index: Kunick, Conrad; Lauenroth, Kathrin; Leost, Maryse; Meijer, Laurent; Lemcke, Thomas Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 2 p. 413 - 416

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Citation Number: 148

Abstract

Kenpaullone derivatives with a modified parent ring system were synthesized in order to develop kinase inhibitors with enhanced selectivity. Among the novel structures, 1- azakenpaullone was found to act as a selective GSK-3β versus CDK1 inhibitor. The charge distribution within the 1-azakenpaullone molecule is discussed as a possible explanation for the enhanced GSK-3β selectivity of 1-azakenpaullone compared to other paullone ...