Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3

  • Bioorg Med Chem Lett. 2004 Jan 19;14(2):343-6. doi: 10.1016/j.bmcl.2003.11.008.
Eddy W Yue  1 ,  Susan V DiMeo ,  C Anne Higley ,  Jay A Markwalder ,  Catherine R Burton ,  Pamela A Benfield ,  Robert H Grafstrom ,  Sarah Cox ,  Jodi K Muckelbauer ,  Angela M Smallwood ,  Haiying Chen ,  Chong Hwan Chang ,  George L Trainor ,  Steven P Seitz
Affiliations
  • 1. Bristol-Myers Squibb Company, Experimental Station, PO Box 80500, Wilmington, DE 19880-0500, USA. [email protected]
PMID: 14698155 DOI: 10.1016/j.bmcl.2003.11.008
Abstract

New indeno[1,2-c]pyrazol-4-one cyclin dependent kinase inhibitors have been disclosed. The most promising compounds are nanomolar enzyme inhibitors with excellent activity against tumor cells. The most advanced compound retains Cell Culture activity even in the presence of human serum proteins. The most advanced compound did not kill the normal fibroblast line AG1523.

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