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Bioorg Med Chem Lett. 2008 Jan 1;18(1):329-35. Epub 2007 Oct 30.

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

Author information

1
Division of Clinical Pharmacology & Experimental Therapeutics, Department of Medicine, Columbia University, 630 West 168th Street, New York, NY 10032, USA.

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.

PMID:
18024113
PMCID:
PMC2275118
DOI:
10.1016/j.bmcl.2007.10.100
[Indexed for MEDLINE]
Free PMC Article

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