title: Design and structure-activity relationship of heterocyclic analogs of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones as inhibitors of receptor tyrosine kinases.
abstract: Herein are described a series of novel heterocyclic analogs of the 4-amino-3-benzimidazol-2-ylhydroquinolin-2-one scaffold. These compounds are potent inhibitors of receptor tyrosine kinases and exhibit favorable pharmacokinetic profiles. The synthesis and SAR of these compounds are described.
authors.affiliation: Small Molecule Drug Discovery, Biopharma Division, Chiron Corporation, 4560 Horton Street, Emeryville, CA 94608, USA.
authors.forename: Kelly
authors.initials: K
authors.lastname: Frazier
authors.forename: Elisa
authors.initials: E
authors.lastname: Jazan
authors.forename: Christopher M
authors.initials: CM
authors.lastname: McBride
authors.forename: Sabina
authors.initials: S
authors.lastname: Pecchi
authors.forename: Paul A
authors.initials: PA
authors.lastname: Renhowe
authors.forename: Cynthia M
authors.initials: CM
authors.lastname: Shafer
authors.forename: Clarke
authors.initials: C
authors.lastname: Taylor
authors.forename: Dirksen
authors.initials: D
authors.lastname: Bussiere
authors.forename: Molly Min
authors.initials: MM
authors.lastname: He
authors.forename: Johanna M
authors.initials: JM
authors.lastname: Jansen
authors.forename: Gena
authors.initials: G
authors.lastname: Lapointe
authors.forename: Sylvia
authors.initials: S
authors.lastname: Ma
authors.forename: Jayesh
authors.initials: J
authors.lastname: Vora
authors.forename: Marion
authors.initials: M
authors.lastname: Wiesmann
mesh_terms: D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D006873:Hydroquinones / Q000138:chemical synthesis* / Q000494:pharmacology; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D001562:Benzimidazoles; D004791:Enzyme Inhibitors; D006571:Heterocyclic Compounds; D006873:Hydroquinones; D020794:Receptor Protein-Tyrosine Kinases