Synthesis of pyrimidinopyridine-triazene conjugates targeted to abl tyrosine kinase

Bioorg Med Chem Lett. 2003 Oct 6;13(19):3297-300. doi: 10.1016/s0960-894x(03)00553-5.

Abstract

The synthesis and abl tyrosine kinase inhibitory activities of alkyltriazenes conjugated to phenylaminopyrimidines are described. Significant abl inhibitory activities were observed only when a benzamido spacer was inserted between the 1,2,3-triazene chain and the 2-phenyaminopyridopyrimidine moiety.

MeSH terms

  • Drug Delivery Systems / methods*
  • Enzyme Inhibitors / administration & dosage
  • Enzyme Inhibitors / chemical synthesis
  • Fusion Proteins, bcr-abl
  • Protein-Tyrosine Kinases / antagonists & inhibitors*
  • Protein-Tyrosine Kinases / metabolism
  • Pyridines / administration & dosage
  • Pyridines / chemical synthesis*
  • Pyrimidinones / administration & dosage
  • Pyrimidinones / chemical synthesis*
  • Triazenes / administration & dosage
  • Triazenes / chemical synthesis*

Substances

  • Enzyme Inhibitors
  • Pyridines
  • Pyrimidinones
  • Triazenes
  • Protein-Tyrosine Kinases
  • Fusion Proteins, bcr-abl