Structure-activity relationships of a novel class of Src SH2 inhibitors.
The structure-activity relationships (SAR) of a novel class of Src SH2 inhibitors are described. Variation at the pY+1 and pY+3 side chain positions using 2,4- and 2,5-substituted thiazoles and 1,2,4-oxadiazoles as scaffolds resulted in inhibitors that bound as well as the standard tetrapeptide Ac-pYEEI-NH2.
Buchanan
J L
JL
ARIAD Pharmaceuticals, Inc., Cambridge, Massachusetts 02139-4234, USA. john.buchanan@ariad.com
Vu
C B
CB
Merry
T J
TJ
Corpuz
E G
EG
Pradeepan
S G
SG
Mani
U N
UN
Yang
M
M
Plake
H R
HR
Varkhedkar
V M
VM
Lynch
B A
BA
MacNeil
I A
IA
Loiacono
K A
KA
Tiong
C L
CL
Holt
D A
DA
D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry* / Q000494:pharmacology*; D018909:src Homology Domains
D013844:Thiazoles