Identification of N-(quinolin-8-yl) benzenesulfonamides as agents capable of down-regulating NFκB activity within two separate high-throughput screens of NFκB …

…, YQ Zhang, A Rinderspacher, W Huang, G Gong…

Index: Xie, Yuli; Deng, ShiXian; Thomas, Craig J.; Liu, Yidong; Zhang, Ya-Qin; Rinderspacher, Alison; Huang, Wenwei; Gong, Gangli; Wyler, Michael; Cayanis, Efithia; Aulner, Nathalie; Toebben, Udo; Chung, Caty; Pampou, Sergey; Southall, Noel; Vidovic, Dusica; Schuerer, Stephan; Branden, Lars; Davis, R. Eric; Staudt, Louis M.; Inglese, James; Austin, Christopher P.; Landry, Donald W.; Smith, Deborah H.; Auld, Douglas S. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 1 p. 329 - 335

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Citation Number: 17

Abstract

We describe here a series of N-(quinolin-8-yl) benzenesulfonamides capable of suppressing the NFκB 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 NFκB activation and expanded upon through analogue synthesis. The series exhibited potencies in the cell-based assays at as low as ...