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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.
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.
Affiliation
  • Pippione AC; Department of Science and Drug Technology , University of Torino , via Pietro Giuria 9 , 10125 Torino , Italy.
  • Federico A; Department of Science and Drug Technology , University of Torino , via Pietro Giuria 9 , 10125 Torino , Italy.
  • Ducime A; Department of Science and Drug Technology , University of Torino , via Pietro Giuria 9 , 10125 Torino , Italy.
  • Sainas S; Department of Science and Drug Technology , University of Torino , via Pietro Giuria 9 , 10125 Torino , Italy.
  • Boschi D; Department of Science and Drug Technology , University of Torino , via Pietro Giuria 9 , 10125 Torino , Italy.
  • Barge A; Department of Science and Drug Technology , University of Torino , via Pietro Giuria 9 , 10125 Torino , Italy.
  • Lupino E; Department of Oncology , University of Torino , via Michelangelo 27/B , 10126 Torino , Italy.
  • Piccinini M; Department of Oncology , University of Torino , via Michelangelo 27/B , 10126 Torino , Italy.
  • Kubbutat M; ProQinase GmbH , Breisacher Str. 117 , 79106 Freiburg , Germany.
  • Contreras JM; Prestwick Chemical , 220 Boulevard Gonthier d'Andernach , 67400 Illkirch , France.
  • Morice C; Prestwick Chemical , 220 Boulevard Gonthier d'Andernach , 67400 Illkirch , France.
  • Al-Karadaghi S; SARomics Biostructures and Department of Biochemistry & Structural Biology , Lund University , Lund , Sweden.
  • Lolli ML; Department of Science and Drug Technology , University of Torino , via Pietro Giuria 9 , 10125 Torino , Italy.
Medchemcomm ; 8(9): 1850-1855, 2017 Sep 01.
Article in En | MEDLINE | ID: mdl-30108896
ABSTRACT
The NF-κB signaling pathway is a validated oncological target. Here, we applied scaffold hopping to IMD-0354, a presumed IKKß 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 IKKß enzyme assays.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Language: En Journal: Medchemcomm Year: 2017 Type: Article Affiliation country: Italy
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Full text: 1 Collection: 01-internacional Database: MEDLINE Language: En Journal: Medchemcomm Year: 2017 Type: Article Affiliation country: Italy