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Discovery of SARxxxx92, a pan-PIM kinase inhibitor, efficacious in a KG1 tumor model.

Abstract：

:N-substituted azaindoles were discovered as potent pan-PIM inhibitors. Lead optimization, guided by structure and focused on physico-chemical properties allowed us to solve inherent hERG and permeability liabilities, and provided compound 27, which subsequently impacted KG-1 tumor growth in a mouse model.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Barberis C,Erdman P,Czekaj M,Fire L,Pribish J,Tserlin E,Maniar S,Batchelor JD,Liu J,Patel VF,Hebert A,Levit M,Wang A,Sun F,Huang SA

doi

10.1016/j.bmcl.2020.127625

subject

Has Abstract

pub_date

2020-12-01 00:00:00

pages

127625

issue

23

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(20)30736-8

journal_volume

30

pub_type

杂志文章

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