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

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.

The preparation and Src kinase inhibitory activity of a series of 4-anilino-7-thienyl-3-quinolinecarbonitriles is reported.Figure optionsDownload as PowerPoint slide