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

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

Affiliation

  • 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.

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