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

  • Bioorg Med Chem Lett. 2010 Aug 15;20(16):4940-4. doi: 10.1016/j.bmcl.2010.06.024.
David P Power  1 ,  Olivier Lozach ,  Laurent Meijer ,  David H Grayson ,  Stephen J Connon
Affiliations
  • 1. Centre for Synthesis and Chemical Biology, School of Chemistry, University of Dublin, Trinity College, Dublin 2, Ireland.
PMID: 20621478 DOI: 10.1016/j.bmcl.2010.06.024
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.