Discovery of N-substituted 7-azaindoles as Pan-PIM kinase inhibitors - Lead series identification - Part II.

Claude Barberis, Neil Moorcroft,James Pribish, Elina Tserlin,Alexandre Gross,Mark Czekaj,Matthieu Barrague,Paul Erdman,Tahir Majid,Joseph Batchelor,Mikhail Levit,Andrew Hebert, Liduo Shen,Sandra Moreno-Mazza,Anlai Wang

Bioorganic & Medicinal Chemistry Letters（2017）

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摘要

N-Substituted azaindoles have been discovered as pan-PIM kinase inhibitors. Initial SAR, early ADME and PK/PD data of a series of compounds is described and led to the identification of promising pan-PIM inhibitors which validated our interest in the 7-azaindole scaffold and led us to pursue the identification of a clinical candidate.

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关键词

Pan-PIM kinases,X-ray crystallography,AML,PK/PD,Hit-to-Lead,Small molecule inhibitor,Cancer

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