3,5-Disubstituted-indole-7-carboxamides as IKKβ Inhibitors: Optimization of Oral Activity via the C3 Substituent.

ACS medicinal chemistry letters（2018）

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摘要

IκB kinase β (IKKβ or IKK2) is a key regulator of nuclear factor kappa B (NF-κB) and has received attention as a therapeutic target. Herein we report on the optimization of a series of 3,5-disubstituted-indole-7-carboxamides for oral activity. In doing so, we focused attention on potency, ligand efficiency (LE), and physicochemical properties and have identified compounds and ()- as having robust in vivo activity.

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关键词

I kappa B Kinase beta,IKK beta,IKK2,NF-kappa B,Indole carboxamide,Cyclic sulfone,LPS neutrophilia,LPS-TNF alpha,Dog segmental LPS challenge

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