1. Academic Validation
  2. 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

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

Affiliation

  • 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. mark.wittman@bms.com
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.

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