Novel 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase

Mark D Wittman; Balu Balasubramanian; Karen Stoffan; Upender Velaparthi; Pieying Liu; Subramaniam Krishnanathan; Joan Carboni; Aixin Li; Ann Greer; Ricardo Attar; Marco Gottardis; Chiehying Chang; Bruce Jacobson; Yax Sun; Steven Hansel; Mary Zoeckler; Dolatrai M Vyas

doi:10.1016/j.bmcl.2006.11.041

Novel 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase

Bioorg Med Chem Lett. 2007 Feb 15;17(4):974-7. doi: 10.1016/j.bmcl.2006.11.041. Epub 2006 Nov 17.

Authors

Mark D Wittman¹, Balu Balasubramanian, Karen Stoffan, Upender Velaparthi, Pieying Liu, Subramaniam Krishnanathan, Joan Carboni, Aixin Li, Ann Greer, Ricardo Attar, Marco Gottardis, Chiehying Chang, Bruce Jacobson, Yax Sun, Steven Hansel, Mary Zoeckler, Dolatrai M Vyas

Affiliation

¹ Department of Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5100, Wallingford, CT 06492-7660, USA. mark.wittman@bms.com

PMID: 17187980
DOI: 10.1016/j.bmcl.2006.11.041

Abstract

A novel class of 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase is described. This report discusses the SAR of 4-(2-hydroxy-2-phenylethylamino)-substituted pyridones with improved IGF-1R potency.

MeSH terms

Animals
Baculoviridae / enzymology
Benzimidazoles / chemical synthesis*
Benzimidazoles / pharmacology*
Cell Line
Cell Proliferation / drug effects
Indicators and Reagents
Insulin-Like Growth Factor I / antagonists & inhibitors*
Mice
Models, Molecular
Phosphotransferases / antagonists & inhibitors*
Pyridones / pharmacology
Structure-Activity Relationship
Thymidine / metabolism

Substances

BMS 536924
Benzimidazoles
Indicators and Reagents
Pyridones
Insulin-Like Growth Factor I
Phosphotransferases
Thymidine