Novel 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase.
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.
Wittman
Mark D
MD
Department of Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5100, Wallingford, CT 06492-7660, USA. mark.wittman@bms.com
Balasubramanian
Balu
B
Stoffan
Karen
K
Velaparthi
Upender
U
Liu
Pieying
P
Krishnanathan
Subramaniam
S
Carboni
Joan
J
Li
Aixin
A
Greer
Ann
A
Attar
Ricardo
R
Gottardis
Marco
M
Chang
Chiehying
C
Jacobson
Bruce
B
Sun
Yax
Y
Hansel
Steven
S
Zoeckler
Mary
M
Vyas
Dolatrai M
DM
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
C504983:BMS 536924; D001562:Benzimidazoles; D007202:Indicators and Reagents; D011728:Pyridones; D007334:Insulin-Like Growth Factor I; D010770:Phosphotransferases; D013936:Thymidine