Jump to main content
Jump to site search

Issue 9, 2017
Previous Article Next Article

4-Hydroxy-N-[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide: a novel inhibitor of the canonical NF-κB cascade

Author affiliations

Abstract

The NF-κB signaling pathway is a validated oncological target. Here, we applied scaffold hopping to IMD-0354, a presumed IKKβ inhibitor, and identified 4-hydroxy-N-[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide (4) as a nM-inhibitor of the NF-κB pathway. However, both 4 and IMD-0354, being potent inhibitors of the canonical NF-κB pathway, were found to be inactive in human IKKβ enzyme assays.

Graphical abstract: 4-Hydroxy-N-[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide: a novel inhibitor of the canonical NF-κB cascade

Back to tab navigation

Supplementary files

Publication details

The article was received on 30 May 2017, accepted on 22 Aug 2017 and first published on 25 Aug 2017


Article type: Research Article
DOI: 10.1039/C7MD00278E
Citation: Med. Chem. Commun., 2017,8, 1850-1855
  •   Request permissions

    4-Hydroxy-N-[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide: a novel inhibitor of the canonical NF-κB cascade

    A. C. Pippione, A. Federico, A. Ducime, S. Sainas, D. Boschi, A. Barge, E. Lupino, M. Piccinini, M. Kubbutat, J. Contreras, C. Morice, S. Al-Karadaghi and M. L. Lolli, Med. Chem. Commun., 2017, 8, 1850
    DOI: 10.1039/C7MD00278E

Search articles by author

Spotlight

Advertisements