2. Academic Validation
  3. Inhibition of Src kinase activity by 7-ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of SKS-927

Inhibition of Src kinase activity by 7-ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of SKS-927

  • Bioorg Med Chem Lett. 2007 Mar 1;17(5):1358-61. doi: 10.1016/j.bmcl.2006.11.077.
Diane H Boschelli 1,  Ana Carolina Barrios Sosa,  Jennifer M Golas,  Frank Boschelli
Affiliations

Affiliation

  • 1 Wyeth Research, Chemical and Screening Sciences, 401 N. Middletown Road, Pearl River, NY 10965, USA. bosched@wyeth.com
PMID: 17188862 DOI: 10.1016/j.bmcl.2006.11.077
Abstract

Of a series of 7-ethynyl-3-quinolinecarbonitriles, the most potent Src inhibitory activity was observed with 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[4-(4-methylpiperazin-1-yl)but-1-ynyl]-3-quinolinecarbonitrile (SKS-927). Variation of the solubilizing amine tail or removal of the methoxy group from either C-6 of the quinoline core or C-5 of the aniline headpiece led to reduced activity.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-10188
    Src Kinase Inhibitor