Details

Autor(en) / Beteiligte

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

Titel

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

Ist Teil von

• MedChemComm, 2017-09, Vol.8 (9), p.1850-1855

Ort / Verlag

England

Erscheinungsjahr

2017

Link zum Volltext

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• 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- -[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide ( ) as a nM-inhibitor of the NF-κB pathway. However, both and IMD-0354, being potent inhibitors of the canonical NF-κB pathway, were found to be inactive in human IKKβ enzyme assays.