Inhibition of Src kinase activity by 4-anilino-7-thienyl-3-quinolinecarbonitriles

Bioorg Med Chem Lett. 2002 Aug 5;12(15):2011-4. doi: 10.1016/s0960-894x(02)00302-5.

Abstract

Based on a screening lead from a yeast-based assay to identify Src family kinase inhibitors, a series of 4-anilino-7-thienyl-3-quinolinecarbonitriles was prepared. When the thiophene ring was substituted with a water-solubilizing group in a 2,5-, 3,5- or 2,4-pattern, potent inhibition of Src kinase activity was observed.

MeSH terms

  • Aniline Compounds / chemistry
  • Aniline Compounds / pharmacology*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Inhibitory Concentration 50
  • Isomerism
  • Nitriles / chemistry
  • Nitriles / pharmacology*
  • Quinolines / chemistry
  • Quinolines / pharmacology*
  • Saccharomyces cerevisiae / drug effects
  • Saccharomyces cerevisiae / enzymology
  • Solubility
  • Structure-Activity Relationship
  • Thiophenes / chemistry
  • src-Family Kinases / antagonists & inhibitors*

Substances

  • Aniline Compounds
  • Enzyme Inhibitors
  • Nitriles
  • Quinolines
  • Thiophenes
  • src-Family Kinases