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

Forskningsoutput: TidskriftsbidragArtikel i vetenskaplig tidskriftPeer review

Sammanfattning

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.

Originalspråkengelska
Sidor (från-till)1850-1855
Antal sidor6
TidskriftMedChemComm
Volym8
Nummer9
DOI
StatusPublished - 2017

Ämnesklassifikation (UKÄ)

  • Läkemedelskemi
  • Cancer och onkologi

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