Investigation of the effect of varying the 4-anilino and 7-alkoxy groups of 3-quinolinecarbonitriles on the inhibition of Src kinase activity

  • Bioorg Med Chem Lett. 2003 Nov 3;13(21):3797-800. doi: 10.1016/j.bmcl.2003.07.001.
Diane H Boschelli  1 ,  Fei Ye ,  Biqi Wu ,  Yanong D Wang ,  Ana Carolina Barrios Sosa ,  Deanna Yaczko ,  Dennis Powell ,  Jennifer M Golas ,  Judy Lucas ,  Frank Boschelli
Affiliations
  • 1. Chemical and Screening Sciences, Wyeth Research, 401 N. Middletown Road, Pearl River, NY 10965, USA. [email protected]
PMID: 14552782 DOI: 10.1016/j.bmcl.2003.07.001
Abstract

Several 7-alkoxy-4-anilino-3-quinolinecarbonitriles were synthesized and evaluated for Src kinase inhibitory activity. Optimal inhibition of both Src enzymatic and cellular activity was seen with analogues having a 2,4-dichloro-5-methoxyaniline group at C-4. Compound 18, which has a 1-methylpiperidinemethoxy group at C-7, showed in vivo activity in a xenograft model.