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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Τόπος έκδοσης:ACS Med Chem Lett
Κύριοι συγγραφείς: 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.
Μορφή: Artigo
Γλώσσα:Inglês
Έκδοση: American Chemical Society 2018
Διαθέσιμο Online: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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