Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones

…, O Lozach, L Meijer, DH Grayson, SJ Connon

Index: Power, David P.; Lozach, Olivier; Meijer, Laurent; Grayson, David H.; Connon, Stephen J. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 16 p. 4940 - 4944

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Citation Number: 16

Abstract

A remarkably concise, chromatography-free route to the parent compound of the paullone family of cyclin-dependent kinase (CDK) inhibitors is reported. A similar strategy allowed the synthesis of the hitherto missing 9-azapaullone and its protonated, N-oxidised and N- alkylated derivatives. Screening studies identified an active and strongly selective inhibitor of CDK9/cyclin T.