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

Claude Barberis,James Pribish, Elina Tserlin,Alexandre Gross,Mark Czekaj,Matthieu Barragué,Paul Erdman, Sachin Maniar,John Jiang, Luke Fire,Vinod Patel,Andrew Hebert,Mikhail Levit,Anlai Wang,Frank Sun,Shih-Min A Huang

Bioorganic & Medicinal Chemistry Letters（2019）

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摘要

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.

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关键词

Lead,Pan-PIM kinases,AML,PK/PD,Tumor growth inhibition,Cancer

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