Nonpeptidic SH2 inhibitors of the tyrosine kinase ZAP-70

C B Vu; E G Corpuz; S G Pradeepan; S Violette; C Bartlett; T K Sawyer

doi:10.1016/s0960-894x(99)00524-7

Nonpeptidic SH2 inhibitors of the tyrosine kinase ZAP-70

Bioorg Med Chem Lett. 1999 Oct 18;9(20):3009-14. doi: 10.1016/s0960-894x(99)00524-7.

Authors

C B Vu¹, E G Corpuz, S G Pradeepan, S Violette, C Bartlett, T K Sawyer

Affiliation

¹ ARIAD Pharmaceuticals, Inc., Cambridge MA 02139-4234, USA.

PMID: 10571165
DOI: 10.1016/s0960-894x(99)00524-7

Abstract

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.

MeSH terms

Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Fluorescence Polarization
Protein Binding
Protein-Tyrosine Kinases / antagonists & inhibitors*
ZAP-70 Protein-Tyrosine Kinase
src Homology Domains*

Substances

Enzyme Inhibitors
Protein-Tyrosine Kinases
ZAP-70 Protein-Tyrosine Kinase