Inhibition of Src kinase activity by 4-anilino-5,10-dihydro-pyrimido[4,5-b]quinolines

Bioorg Med Chem Lett. 2003 Sep 15;13(18):2977-80. doi: 10.1016/s0960-894x(03)00628-0.

Abstract

4-(2,4-Dichloro-5-methoxy)anilino-5,10-dihydropyrimido[4,5-b]quinolines are potent inhibitors of Src kinase and Src cellular activity while having no effect on Fyn cellular activity. The corresponding 4-(2,4-dichloro-5-methoxy)anilino-pyrimido[4,5-b]quinolines are much less effective Src inhibitors.

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Cell Division / drug effects
  • Cell Line, Transformed
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / pharmacology
  • Fibroblasts / cytology
  • Humans
  • Inhibitory Concentration 50
  • Quinolines / chemical synthesis*
  • Quinolines / pharmacology
  • Structure-Activity Relationship
  • src-Family Kinases / antagonists & inhibitors*

Substances

  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Quinolines
  • src-Family Kinases