The synthesis and structure-activity relationship (SAR) trends of a new class of N-(azacycloalkyl)bisindolylmaleimides 1, acyclic derivatives of staurosporine, is described. The representative compound for this series (1e) exhibits an IC 5 0 of 40-50 nM against the human PKCβ 1 and PKCβ 2 isozymes and selectively inhibits the PKCβ isozymes in comparison to other PKC isozymes (α, γ, δ, , λ, and η). The series is also kinase selective for PKC in comparison to other ATP-dependent kinases. A comparison of the PKC isozyme and kinase activity of the series is made to the kinase inhibitor staurosporine.