title: Novel 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase.
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.
authors.affiliation: Department of Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5100, Wallingford, CT 06492-7660, USA. mark.wittman@bms.com
authors.forename: Mark D
authors.initials: MD
authors.lastname: Wittman
authors.forename: Balu
authors.initials: B
authors.lastname: Balasubramanian
authors.forename: Karen
authors.initials: K
authors.lastname: Stoffan
authors.forename: Upender
authors.initials: U
authors.lastname: Velaparthi
authors.forename: Pieying
authors.initials: P
authors.lastname: Liu
authors.forename: Subramaniam
authors.initials: S
authors.lastname: Krishnanathan
authors.forename: Joan
authors.initials: J
authors.lastname: Carboni
authors.forename: Aixin
authors.initials: A
authors.lastname: Li
authors.forename: Ann
authors.initials: A
authors.lastname: Greer
authors.forename: Ricardo
authors.initials: R
authors.lastname: Attar
authors.forename: Marco
authors.initials: M
authors.lastname: Gottardis
authors.forename: Chiehying
authors.initials: C
authors.lastname: Chang
authors.forename: Bruce
authors.initials: B
authors.lastname: Jacobson
authors.forename: Yax
authors.initials: Y
authors.lastname: Sun
authors.forename: Steven
authors.initials: S
authors.lastname: Hansel
authors.forename: Mary
authors.initials: M
authors.lastname: Zoeckler
authors.forename: Dolatrai M
authors.initials: DM
authors.lastname: Vyas
mesh_terms: D000818:Animals; D016367:Baculoviridae / Q000201:enzymology; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D007202:Indicators and Reagents; D007334:Insulin-Like Growth Factor I / Q000037:antagonists & inhibitors*; D051379:Mice; D008958:Models, Molecular; D010770:Phosphotransferases / Q000037:antagonists & inhibitors*; D011728:Pyridones / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013936:Thymidine / Q000378:metabolism
chemical_list: C504983:BMS 536924; D001562:Benzimidazoles; D007202:Indicators and Reagents; D011728:Pyridones; D007334:Insulin-Like Growth Factor I; D010770:Phosphotransferases; D013936:Thymidine