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

Yuli Xie, 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, Dušica Vidović, Stephan Schürer, Lars Branden, R. Eric Davis, Louis M. Staudt & 5 others James Inglese, Christopher P. Austin, Donald W. Landry, Deborah H. Smith, Douglas S. Auld

Research output: Contribution to journalArticle

14 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)329-335
Number of pages7
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number1
DOIs
StatePublished - Jan 1 2008
Externally publishedYes

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Assays
Chemical activation
Throughput
Molecules
benzenesulfonamide

Keywords

  • NFκB inhibitor

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFκB activity within two separate high-throughput screens of NFκB activation. / Xie, Yuli; Deng, ShiXian; Thomas, Craig J.; Liu, Yidong; Zhang, Ya Qin; Rinderspacher, Alison; Huang, Wenwei; Gong, Gangli; Wyler, Michael; Cayanis, Efithia; Aulner, Nathalie; Többen, Udo; Chung, Caty; Pampou, Sergey; Southall, Noel; Vidović, Dušica; Schürer, Stephan; Branden, Lars; Davis, R. Eric; Staudt, Louis M.; Inglese, James; Austin, Christopher P.; Landry, Donald W.; Smith, Deborah H.; Auld, Douglas S.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 18, No. 1, 01.01.2008, p. 329-335.

Research output: Contribution to journalArticle

Xie, Y, Deng, S, Thomas, CJ, Liu, Y, Zhang, YQ, Rinderspacher, A, Huang, W, Gong, G, Wyler, M, Cayanis, E, Aulner, N, Többen, U, Chung, C, Pampou, S, Southall, N, Vidović, D, Schürer, S, Branden, L, Davis, RE, Staudt, LM, Inglese, J, Austin, CP, Landry, DW, Smith, DH & Auld, DS 2008, 'Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFκB activity within two separate high-throughput screens of NFκB activation', Bioorganic and Medicinal Chemistry Letters, vol. 18, no. 1, pp. 329-335. https://doi.org/10.1016/j.bmcl.2007.10.100
Xie, Yuli ; Deng, ShiXian ; Thomas, Craig J. ; Liu, Yidong ; Zhang, Ya Qin ; Rinderspacher, Alison ; Huang, Wenwei ; Gong, Gangli ; Wyler, Michael ; Cayanis, Efithia ; Aulner, Nathalie ; Többen, Udo ; Chung, Caty ; Pampou, Sergey ; Southall, Noel ; Vidović, Dušica ; Schürer, Stephan ; Branden, Lars ; Davis, R. Eric ; Staudt, Louis M. ; Inglese, James ; Austin, Christopher P. ; Landry, Donald W. ; Smith, Deborah H. ; Auld, Douglas S. / Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFκB activity within two separate high-throughput screens of NFκB activation. In: Bioorganic and Medicinal Chemistry Letters. 2008 ; Vol. 18, No. 1. pp. 329-335.
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AU - Zhang, Ya Qin

AU - Rinderspacher, Alison

AU - Huang, Wenwei

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AU - Branden, Lars

AU - Davis, R. Eric

AU - Staudt, Louis M.

AU - Inglese, James

AU - Austin, Christopher P.

AU - Landry, Donald W.

AU - Smith, Deborah H.

AU - Auld, Douglas S.

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