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Discovery of 6-aryl-7-alkoxyisoquinoline inhibitors of IkappaB kinase-beta (IKK-beta).
Christopher, John A; Bamborough, Paul; Alder, Catherine; Campbell, Amanda; Cutler, Geoffrey J; Down, Kenneth; Hamadi, Ahmed M; Jolly, Adrian M; Kerns, Jeffrey K; Lucas, Fiona S; Mellor, Geoffrey W; Miller, David D; Morse, Mary A; Pancholi, Kiritkant D; Rumsey, William; Solanke, Yemisi E; Williamson, Rick.
J Med Chem ; 52(9): 3098-102, 2009 May 14.
Article in English | MEDLINE | ID: mdl-19348415

ABSTRACT

The identification and progression of a potent and selective series of isoquinoline inhibitors of IkappaB kinase-beta (IKK-beta) are described. Hit-generation chemistry based on IKK-beta active-site knowledge yielded a weakly potent but tractable chemotype that was rapidly progressed into a series with robust enzyme and cellular activity and significant selectivity over IKK-alpha.


Subject(s)
Drug Discovery , I-kappa B Kinase/antagonists & inhibitors , Isoquinolines/chemistry , Isoquinolines/pharmacology , Protein Kinase Inhibitors/chemistry , Protein Kinase Inhibitors/pharmacology , Humans , I-kappa B Kinase/chemistry , I-kappa B Kinase/metabolism , Inhibitory Concentration 50 , Isoquinolines/metabolism , Models, Molecular , Molecular Conformation , Protein Kinase Inhibitors/metabolism
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