Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.
We report the discovery and preliminary SAR studies of a series of structurally novel benzotriazine core based small molecules as inhibitors of Src kinase. To the best of our knowledge, benzotriazine template based compounds have not been reported as kinase inhibitors. The 3-(2-(1-pyrrolidinyl)ethoxy)phenyl analogue (43) was identified as one of the most potent inhibitors of Src kinase.
Noronha
Glenn
G
TargeGen, Inc., 9380 Judicial Drive, San Diego, CA 92121, USA. noronha@targegen.com
Barrett
Kathy
K
Cao
Jianguo
J
Dneprovskaia
Elena
E
Fine
Richard
R
Gong
Xianchang
X
Gritzen
Colleen
C
Hood
John
J
Kang
Xinshan
X
Klebansky
Boris
B
Li
G
G
Liao
W
W
Lohse
Dan
D
Mak
Chi Ching
CC
McPherson
Andrew
A
Palanki
Moorthy S S
MS
Pathak
Ved P
VP
Renick
Joel
J
Soll
Richard
R
Splittgerber
Ute
U
Wrasidlo
Wolfgang
W
Zeng
Binqi
B
Zhao
Ningning
N
Zhou
Y
Y
D006801:Humans; D016392:Proto-Oncogene Proteins pp60(c-src) / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014227:Triazines / Q000494:pharmacology*
D014227:Triazines; D016392:Proto-Oncogene Proteins pp60(c-src)