4-Hydroxy-N-[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide: a novel inhibitor of the canonical NF-κB cascade†,10.1039/C7MD00278E

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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†

Agnese C. Pippione,Antonella Federico,Alex Ducime,Stefano Sainas,Donatella Boschi,Alessandro Barge,Elisa Lupino,Marco Piccinini,Michael Kubbutat,Jean-Marie Contreras,Christophe Morice,Salam Al-Karadaghi,Marco L. Lolli

MedChemComm Pub Date : 08/25/2017 00:00:00 , DOI:10.1039/C7MD00278E

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.