Synthesis of anilino-monoindolylmaleimides as potent and selective PKCβ inhibitors

Abstract We report herein synthesis of PKCβ-selective inhibitors possessing the novel pharmacophore of anilino-monoindolylmaleimide. Several compounds of this series exhibited IC 50 ’s as low as 50 nM against human PKCβ2. One of the most potent compounds, 6l , inhibited PKCβ1 and PKCβ2 with IC 50 of 21 and 5 nM, respectively, and exhibited selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCe).