Title of article
Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFκB activity within two separate high-throughput screens of NFκB activation
Author/Authors
Yuli Xie، نويسنده , , Shixian Deng، نويسنده , , Craig J. Thomas، نويسنده , , Yidong Liu، نويسنده , , Ya-Qin Zhang، نويسنده , , Alison Rinderspacher، نويسنده , , Wenwei Huang، نويسنده , , Gangli Gong، نويسنده , , Michael Wyler، نويسنده , , Efithia Cayanis، نويسنده , , Nathalie Aulner، نويسنده , , Udo T?bben، نويسنده , , Caty Chung، نويسنده , , Sergey Pampou، نويسنده , , Noel Southall، نويسنده , , Du?ica Vidovi?، نويسنده , , Stephan Schürer، نويسنده , , Lars Branden، نويسنده , , R. Eric Davis، نويسنده , , Louis M. Staudt، نويسنده , , et al.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
7
From page
329
To page
335
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 0.6 μM, and several indications suggest that the targeted activity lies within a common region of the NFκB pathway.
Keywords
NF?B inhibitor
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798973
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