| Literature DB >> 18024113 |
Yuli Xie1, ShiXian Deng, Craig J Thomas, Yidong Liu, Ya-Qin Zhang, Alison Rinderspacher, Wenwei Huang, Gangli Gong, Michael Wyler, Efithia Cayanis, Nathalie Aulner, Udo Többen, Caty Chung, Sergey Pampou, Noel Southall, Dusica Vidović, Stephan Schürer, Lars Branden, R Eric Davis, Louis M Staudt, James Inglese, Christopher P Austin, Donald W Landry, Deborah H Smith, Douglas S Auld.
Abstract
We describe here a series of N-(quinolin-8-yl)benzenesulfonamides capable of suppressing the NFkappaB pathway identified from two high-throughput screens run at two centers of the NIH Molecular Libraries Initiative. These small molecules were confirmed in both primary and secondary assays of NFkappaB activation and expanded upon through analogue synthesis. The series exhibited potencies in the cell-based assays at as low as 0.6 microM, and several indications suggest that the targeted activity lies within a common region of the NFkappaB pathway.Entities:
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Year: 2007 PMID： 18024113 PMCID： PMC2275118 DOI： 10.1016/j.bmcl.2007.10.100
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823