Author/Authors :
Karen Lackey، نويسنده , , Michael Cory، نويسنده , , Ronda Davis، نويسنده , , Stephen V. Frye، نويسنده , , Philip A. Harris، نويسنده , , Robert N. Hunter، نويسنده , , David K. Jung، نويسنده , , O. Bradley McDonald، نويسنده , , Robert W. McNutt، نويسنده , , Michael R. Peel، نويسنده , , Randy D. Rutkowske، نويسنده , , James M. Veal، نويسنده , , Edgar R. Wood، نويسنده ,
Abstract :
A series of benzylidene-1H-indol-2-one (oxindole) derivatives was synthesized and evaluated as cRaf-1 kinase inhibitors. The key features of the molecules were the donor/acceptor motif common to kinase inhibitors and a critical acidic phenol flanked by two substitutions. Diverse 5-position substitutions provided compounds with low nanomolar kinase enzyme inhibition and inhibited the intracellular MAPK pathway.
