Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I

Bioorg Med Chem Lett. 2000 Oct 2;10(19):2167-70. doi: 10.1016/s0960-894x(00)00441-8.

Abstract

Pyrrolo[2,3-d]pyrimidines containing a 5-(4-phenoxyphenyl) substituent are potent and selective inhibitors of Ick in vitro; some compounds are selective for lck over src. Data are shown for two compounds demonstrating that they are potent and selective inhibitors of IL2 production in cells.

MeSH terms

  • Drug Design
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Jurkat Cells
  • Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / antagonists & inhibitors*
  • Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / chemistry
  • Models, Molecular
  • Molecular Structure
  • Proto-Oncogene Proteins pp60(c-src) / antagonists & inhibitors
  • Proto-Oncogene Proteins pp60(c-src) / metabolism
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacology*
  • Pyrroles / chemical synthesis*
  • Pyrroles / chemistry
  • Pyrroles / pharmacology*
  • Receptor Protein-Tyrosine Kinases / antagonists & inhibitors
  • Receptor Protein-Tyrosine Kinases / metabolism
  • Receptor, TIE-2
  • Receptors, Growth Factor / antagonists & inhibitors
  • Receptors, Growth Factor / metabolism
  • Receptors, Vascular Endothelial Growth Factor
  • Substrate Specificity

Substances

  • Enzyme Inhibitors
  • Pyrimidines
  • Pyrroles
  • Receptors, Growth Factor
  • Receptor Protein-Tyrosine Kinases
  • Receptor, TIE-2
  • Receptors, Vascular Endothelial Growth Factor
  • Lymphocyte Specific Protein Tyrosine Kinase p56(lck)
  • Proto-Oncogene Proteins pp60(c-src)