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ID: ALA4371067
Journal: Bioorg Med Chem Lett
Title: Discovery of N-substituted 7-azaindoles as Pan-PIM kinases inhibitors - Lead optimization - Part III.
Authors: Barberis C, Pribish J, Tserlin E, Gross A, Czekaj M, Barragué M, Erdman P, Maniar S, Jiang J, Fire L, Patel V, Hebert A, Levit M, Wang A, Sun F, Huang SA.
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.
CiteXplore: 30553737