title: Discovery and initial SAR of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-ones as inhibitors of insulin-like growth factor 1-receptor (IGF-1R).
abstract: The discovery and synthesis of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like growth factor 1-receptor (IGF-1R) are presented. Installing amine containing side chains at the 4-position of pyridone ring significantly improved the enzyme potency. SAR and biological activity of these compounds is presented.
authors.affiliation: Department of Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. upender.velaparthi@bms.com
authors.forename: Upender
authors.initials: U
authors.lastname: Velaparthi
authors.forename: Mark
authors.initials: M
authors.lastname: Wittman
authors.forename: Peiying
authors.initials: P
authors.lastname: Liu
authors.forename: Karen
authors.initials: K
authors.lastname: Stoffan
authors.forename: Kurt
authors.initials: K
authors.lastname: Zimmermann
authors.forename: Xiaopeng
authors.initials: X
authors.lastname: Sang
authors.forename: Joan
authors.initials: J
authors.lastname: Carboni
authors.forename: Aixin
authors.initials: A
authors.lastname: Li
authors.forename: Ricardo
authors.initials: R
authors.lastname: Attar
authors.forename: Marco
authors.initials: M
authors.lastname: Gottardis
authors.forename: Ann
authors.initials: A
authors.lastname: Greer
authors.forename: ChiehYing Y
authors.initials: CY
authors.lastname: Chang
authors.forename: Bruce L
authors.initials: BL
authors.lastname: Jacobsen
authors.forename: John S
authors.initials: JS
authors.lastname: Sack
authors.forename: Yax
authors.initials: Y
authors.lastname: Sun
authors.forename: David R
authors.initials: DR
authors.lastname: Langley
authors.forename: Balu
authors.initials: B
authors.lastname: Balasubramanian
authors.forename: Dolatrai
authors.initials: D
authors.lastname: Vyas
mesh_terms: D001562:Benzimidazoles; D002460:Cell Line; D006801:Humans; D020128:Inhibitory Concentration 50; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011728:Pyridones; D017526:Receptor, IGF Type 1 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D001562:Benzimidazoles; D011725:Pyridines; D011728:Pyridones; D017526:Receptor, IGF Type 1