Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors

Bioorg Med Chem Lett. 2010 May 1;20(9):2924-7. doi: 10.1016/j.bmcl.2010.03.025. Epub 2010 Mar 7.

Abstract

The 7-alkene-3-quinolinecarbonitrile 20, a potent inhibitor of Src enzymatic and cellular activity with IC(50) values of 2.1 and 58 nM, respectively, had comparable efficacy to bosutinib in a colon tumor xenograft study.

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Humans
  • Mice
  • Mice, Nude
  • Microsomes / metabolism
  • Protein Kinase Inhibitors / chemical synthesis
  • Protein Kinase Inhibitors / chemistry*
  • Protein Kinase Inhibitors / pharmacology
  • Quinolines / chemical synthesis
  • Quinolines / chemistry*
  • Quinolines / pharmacology
  • Xenograft Model Antitumor Assays
  • src-Family Kinases / antagonists & inhibitors*
  • src-Family Kinases / metabolism

Substances

  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • Quinolines
  • src-Family Kinases