title: 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.
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.
authors.affiliation: 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
authors.forename: Mark
authors.initials: M
authors.lastname: Wittman
authors.forename: Joan
authors.initials: J
authors.lastname: Carboni
authors.forename: Ricardo
authors.initials: R
authors.lastname: Attar
authors.forename: Balu
authors.initials: B
authors.lastname: Balasubramanian
authors.forename: Praveen
authors.initials: P
authors.lastname: Balimane
authors.forename: Patrick
authors.initials: P
authors.lastname: Brassil
authors.forename: Francis
authors.initials: F
authors.lastname: Beaulieu
authors.forename: Chiehying
authors.initials: C
authors.lastname: Chang
authors.forename: Wendy
authors.initials: W
authors.lastname: Clarke
authors.forename: Janet
authors.initials: J
authors.lastname: Dell
authors.forename: Jeffrey
authors.initials: J
authors.lastname: Eummer
authors.forename: David
authors.initials: D
authors.lastname: Frennesson
authors.forename: Marco
authors.initials: M
authors.lastname: Gottardis
authors.forename: Ann
authors.initials: A
authors.lastname: Greer
authors.forename: Steven
authors.initials: S
authors.lastname: Hansel
authors.forename: Warren
authors.initials: W
authors.lastname: Hurlburt
authors.forename: Bruce
authors.initials: B
authors.lastname: Jacobson
authors.forename: Subramaniam
authors.initials: S
authors.lastname: Krishnananthan
authors.forename: Francis Y
authors.initials: FY
authors.lastname: Lee
authors.forename: Aixin
authors.initials: A
authors.lastname: Li
authors.forename: Tai-An
authors.initials: TA
authors.lastname: Lin
authors.forename: Peiying
authors.initials: P
authors.lastname: Liu
authors.forename: Carl
authors.initials: C
authors.lastname: Ouellet
authors.forename: Xiaopeng
authors.initials: X
authors.lastname: Sang
authors.forename: Mark G
authors.initials: MG
authors.lastname: Saulnier
authors.forename: Karen
authors.initials: K
authors.lastname: Stoffan
authors.forename: Yax
authors.initials: Y
authors.lastname: Sun
authors.forename: Upender
authors.initials: U
authors.lastname: Velaparthi
authors.forename: Henry
authors.initials: H
authors.lastname: Wong
authors.forename: Zheng
authors.initials: Z
authors.lastname: Yang
authors.forename: Kurt
authors.initials: K
authors.lastname: Zimmermann
authors.forename: Mary
authors.initials: M
authors.lastname: Zoeckler
authors.forename: Dolatrai
authors.initials: D
authors.lastname: Vyas
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001682:Biological Availability; D045744:Cell Line, Tumor; D018360:Crystallography, X-Ray; D004354:Drug Screening Assays, Antitumor; D000882:Haplorhini; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D008958:Models, Molecular; D015394:Molecular Structure; D009368:Neoplasm Transplantation; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011728:Pyridones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D017526:Receptor, IGF Type 1 / Q000037:antagonists & inhibitors*; D011972:Receptor, Insulin / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; C504983:BMS 536924; D001562:Benzimidazoles; D011725:Pyridines; D011728:Pyridones; D017526:Receptor, IGF Type 1; D011972:Receptor, Insulin