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

[Image: see text] 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 p...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Kerns, Jeffrey K., Busch-Petersen, Jakob, Fu, Wei, Boehm, Jeffrey C., Nie, Hong, Muratore, Michael, Bullion, Ann, Lin, Guoliang, Li, Huijie, Davis, Roderick, Lin, Xichen, Lakdawala, Ami S., Cousins, Rick, Field, Rita, Payne, Jeremy, Miller, David D., Bamborough, Paul, Christopher, John A., Baldwin, Ian, Osborn, Ruth R., Yonchuk, John, Webb, Edward, Rumsey, William L.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2018
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6295857/
https://ncbi.nlm.nih.gov/pubmed/30613320
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.8b00291
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