2. Academic Validation
  3. Versatile templates for the development of novel kinase inhibitors: Discovery of novel CDK inhibitors

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

Affiliation

  • 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.

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