Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. Part 4: structure-activity relationships for substituents on the quinazoline moiety of 4-[4-(N-substituted(thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives

Bioorg Med Chem Lett. 2003 Sep 15;13(18):3001-4. doi: 10.1016/s0960-894x(03)00634-6.

Abstract

Here, we investigated the structure-activity relationships of the 6,7-dimethoxyquinazoline moiety. With regard to exploration of positions and varieties of substituents on the quinazoline ring, 6,7-dialkoxy substitution was optimal. This study suggests the possibility of further modifications for this moiety.

MeSH terms

  • Animals
  • Humans
  • Inhibitory Concentration 50
  • Phosphorylation / drug effects
  • Quinazolines / chemical synthesis*
  • Quinazolines / chemistry
  • Quinazolines / pharmacology*
  • Receptors, Platelet-Derived Growth Factor / antagonists & inhibitors*
  • Receptors, Platelet-Derived Growth Factor / metabolism
  • Structure-Activity Relationship

Substances

  • Quinazolines
  • Receptors, Platelet-Derived Growth Factor