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.

Detaljer

Författare
  • 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
Enheter & grupper
Externa organisationer
  • University of Turin
  • ProQinase GmbH
  • Prestwick Chemical PC SAS
Forskningsområden

Ämnesklassifikation (UKÄ) – OBLIGATORISK

  • Läkemedelskemi
  • Cancer och onkologi
Originalspråkengelska
Sidor (från-till)1850-1855
Antal sidor6
TidskriftMedChemComm
Volym8
Utgåva nummer9
StatusPublished - 2017
PublikationskategoriForskning
Peer review utfördJa