Synthesis of anilino-monoindolylmaleimides as potent and selective PKCβ inhibitors

We report herein synthesis of PKCβ-selective inhibitors possessing the novel pharmacophore of anilino-monoindolylmaleimide. Several compounds of this series exhibited IC50’s as low as 50 nM against human PKCβ2. One of the most potent compounds, 6l, inhibited PKCβ1 and PKCβ2 with IC50 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 PKCε).