Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity

  • J Med Chem. 2005 Sep 8;48(18):5639-43. doi: 10.1021/jm050392q.
Mark Wittman  1 ,  Joan Carboni ,  Ricardo Attar ,  Balu Balasubramanian ,  Praveen Balimane ,  Patrick Brassil ,  Francis Beaulieu ,  Chiehying Chang ,  Wendy Clarke ,  Janet Dell ,  Jeffrey Eummer ,  David Frennesson ,  Marco Gottardis ,  Ann Greer ,  Steven Hansel ,  Warren Hurlburt ,  Bruce Jacobson ,  Subramaniam Krishnananthan ,  Francis Y Lee ,  Aixin Li ,  Tai-An Lin ,  Peiying Liu ,  Carl Ouellet ,  Xiaopeng Sang ,  Mark G Saulnier ,  Karen Stoffan ,  Yax Sun ,  Upender Velaparthi ,  Henry Wong ,  Zheng Yang ,  Kurt Zimmermann ,  Mary Zoeckler ,  Dolatrai Vyas
Affiliations
  • 1. Discovery Chemistry, Department of Metabolism and Pharmacokinetics, Department of Computer Aided Drug Design, and Department of Chemical Synthesis, Bristol-Myers Squibb Co, 5 Research Parkway, Wallingford, Connecticut 06492, USA. [email protected]
PMID: 16134929 DOI: 10.1021/jm050392q
Abstract

Compound 3 (BMS-536924), a novel small-molecule inhibitor of the insulin-like growth factor receptor kinase with equal potency against the Insulin Receptor is described. The in vitro and in vivo biological activity of this interesting compound is also reported.

Products