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

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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

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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, Advance Article
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    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, Advance Article , DOI: 10.1039/C7MD00278E

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