Discovery of 6-Aryl-7-alkoxyisoquinoline Inhibitors of IκB Kinase-β (IKK-β)
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- 作者：John A. Christopher ; Paul Bamborough ; Catherine Alder ; Amanda Campbell ; Geoffrey J. Cutler ; Kenneth Down ; Ahmed M. Hamadi ; Adrian M. Jolly ; Jeffrey K. Kerns ; Fiona S. Lucas ; Geoffrey W. Mellor ; David
- 刊名：Journal of Medicinal Chemistry
- 出版年：2009
- 出版时间：May 14, 2009
- 年：2009
- 卷：52
- 期：9
- 页码：3098-3102
- 全文大小：183K
- 年卷期：v.52,no.9(May 14, 2009)
- ISSN：1520-4804
文摘
The identification and progression of a potent and selective series of isoquinoline inhibitors of IκB kinase-β (IKK-β) are described. Hit-generation chemistry based on IKK-β 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-α.