Nonpeptidic SH2 inhibitors of the tyrosine kinase ZAP-70.
The synthesis of a series of 1,2,4-oxadiazole analogs is discussed along with their ZAP-70 SH2 inhibitory activity. The tyrosine moiety in the original series has been replaced with nonpeptidic functional groups without a substantial loss of binding affinity.
Vu
C B
CB
ARIAD Pharmaceuticals, Inc., Cambridge MA 02139-4234, USA.
Corpuz
E G
EG
Pradeepan
S G
SG
Violette
S
S
Bartlett
C
C
Sawyer
T K
TK
D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D005454:Fluorescence Polarization; D011485:Protein Binding; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D051746:ZAP-70 Protein-Tyrosine Kinase; D018909:src Homology Domains
D004791:Enzyme Inhibitors; D011505:Protein-Tyrosine Kinases; D051746:ZAP-70 Protein-Tyrosine Kinase