Discovery of N-substituted 7-azaindoles as Pan-PIM kinases inhibitors – Lead optimization – Part III

Abstract N -substituted azaindoles were discovered as promising pan-PIM inhibitors. Lead optimization is described en route toward the identification of a clinical candidate. Modulation of physico-chemical properties allowed to solve inherent hERG and permeability liabilities. Compound 17 showed tumor growth inhibition in a KG1 tumor-bearing mouse model.