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

  • Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6. doi: 10.1016/j.bmcl.2003.10.062.
Conrad Kunick  1 ,  Kathrin Lauenroth ,  Maryse Leost ,  Laurent Meijer ,  Thomas Lemcke
Affiliations
  • 1. Institut für Pharmazeutische Chemie, Technische Universität Braunschweig, Beethovenstrasse 55, 38106, Braunschweig, Germany. [email protected]
PMID: 14698171 DOI: 10.1016/j.bmcl.2003.10.062
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-3beta versus CDK1 Inhibitor. The charge distribution within the 1-azakenpaullone molecule is discussed as a possible explanation for the enhanced GSK-3beta selectivity of 1-azakenpaullone compared to Other paullone derivatives.

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