1,3-Disubstituted-imidazo[1,5-a]pyrazines as insulin-like growth-factor-I receptor (IGF-IR) inhibitors.
A series of novel 8-amino-1,3-disubstituted-imidazo[1,5-a]pyrazines was designed and synthesized as IGF-IR inhibitors.
Mulvihill
Mark J
MJ
(OSI) Oncology, OSI Pharmaceuticals, Inc., 1 Bioscience Park Drive, Farmingdale, NY 11735, USA. mmulvihill@osip.com
Ji
Qun-Sheng
QS
Werner
Doug
D
Beck
Patricia
P
Cesario
Cara
C
Cooke
Andrew
A
Cox
Matthew
M
Crew
Andrew
A
Dong
Hanqing
H
Feng
Lixin
L
Foreman
K W
KW
Mak
Gilda
G
Nigro
Anthony
A
O'Connor
Matthew
M
Saroglou
Lydia
L
Stolz
Kathryn M
KM
Sujka
Izabela
I
Volk
Brian
B
Weng
Qinghua
Q
Wilkes
Robin
R
D000255:Adenosine Triphosphate / Q000378:metabolism; D000818:Animals; D019540:Area Under Curve; D001665:Binding Sites; D001682:Biological Availability; D018360:Crystallography, X-Ray; D030562:Databases, Protein; D006207:Half-Life; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D051379:Mice; D008958:Models, Molecular; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors; D011719:Pyrazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D017526:Receptor, IGF Type 1 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D007093:Imidazoles; D007202:Indicators and Reagents; D011719:Pyrazines; D000255:Adenosine Triphosphate; D011505:Protein-Tyrosine Kinases; D017526:Receptor, IGF Type 1