2-ARYL-INDOLYL MALEIMIDES - NOVEL AND POTENT INHIBITORS OF PROTEIN-KINASE-C

A new class of protein kinase C (PKC) inhibitors is described. These i nhibitors were derived from the familiar bis-indolyl maleimide series of inhibitors through a structural rearrangement involving transfer of one aryl ring from the maleimide moiety to the C-2 position of the in dole ring remaining attached to that moiety. The resulting compounds a re among the most potent known inhibitors of PKC and also show good se lectivity for PKC in relation to other kinases. The lead compound in t his series possesses antitumor activity in several in vitro and in viv o models.