4-Pyridin-5-yl-2-(3,4,5-trimethoxyphenylamino)pyrimidines: potent and selective inhibitors of ZAP 70

Bioorg Med Chem Lett. 1999 Dec 6;9(23):3351-6. doi: 10.1016/s0960-894x(99)00615-0.

Abstract

Activation of the tyrosine kinase ZAP 70 has been shown to be crucial to the transduction of the T-cell receptor signalling pathway, which leads ultimately to proliferation, cytokine gene expression and T-cell effector functions. A series of 2-phenylaminopyrimidines have been identified as potent and selective inhibitors of ZAP 70.

MeSH terms

  • Phosphorylation
  • Protein-Tyrosine Kinases / antagonists & inhibitors*
  • Protein-Tyrosine Kinases / metabolism
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacology*
  • Signal Transduction
  • ZAP-70 Protein-Tyrosine Kinase

Substances

  • Pyrimidines
  • Protein-Tyrosine Kinases
  • ZAP-70 Protein-Tyrosine Kinase