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ID: ALA1781921

Journal: Bioorg Med Chem Lett

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

Authors: Power DP, Lozach O, Meijer L, Grayson DH, Connon SJ.

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.

CiteXplore: 20621478

DOI: 10.1016/j.bmcl.2010.06.024