Design and structure-activity relationship of heterocyclic analogs of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones as inhibitors of receptor tyrosine kinases.
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.
Frazier
Kelly
K
Small Molecule Drug Discovery, Biopharma Division, Chiron Corporation, 4560 Horton Street, Emeryville, CA 94608, USA.
Jazan
Elisa
E
McBride
Christopher M
CM
Pecchi
Sabina
S
Renhowe
Paul A
PA
Shafer
Cynthia M
CM
Taylor
Clarke
C
Bussiere
Dirksen
D
He
Molly Min
MM
Jansen
Johanna M
JM
Lapointe
Gena
G
Ma
Sylvia
S
Vora
Jayesh
J
Wiesmann
Marion
M
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
D001562:Benzimidazoles; D004791:Enzyme Inhibitors; D006571:Heterocyclic Compounds; D006873:Hydroquinones; D020794:Receptor Protein-Tyrosine Kinases