Versatile templates for the development of novel kinase inhibitors: Discovery of novel CDK inhibitors

  • Bioorg Med Chem Lett. 2007 Nov 15;17(22):6216-9. doi: 10.1016/j.bmcl.2007.09.018.
Michael P Dwyer  1 ,  Kamil Paruch ,  Carmen Alvarez ,  Ronald J Doll ,  Kerry Keertikar ,  Jose Duca ,  Thierry O Fischmann ,  Alan Hruza ,  Vincent Madison ,  Emma Lees ,  David Parry ,  Wolfgang Seghezzi ,  Nicole Sgambellone ,  Frances Shanahan ,  Derek Wiswell ,  Timothy J Guzi
Affiliations
  • 1. Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. [email protected]
PMID: 17904366 DOI: 10.1016/j.bmcl.2007.09.018
Abstract

A series of four bicyclic cores were prepared and evaluated as cyclin-dependent kinase-2 (CDK2) inhibitors. From the in-vitro and cell-based analysis, the pyrazolo[1,5-a]pyrimidine core (represented by 9) emerged as the superior core for further elaboration in the identification of novel CDK2 inhibitors.