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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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.

I: MedChemComm, Vol. 8, Nr. 9, 2017, s. 1850-1855.

Forskningsoutput: TidskriftsbidragArtikel i vetenskaplig tidskrift

Harvard

Pippione, AC, Federico, A, Ducime, A, Sainas, S, Boschi, D, Barge, A, Lupino, E, Piccinini, M, Kubbutat, M, Contreras, JM, Morice, C, Al-Karadaghi, S & Lolli, ML 2017, '4-Hydroxy-N -[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide: A novel inhibitor of the canonical NF-κB cascade', MedChemComm, vol. 8, nr. 9, s. 1850-1855. https://doi.org/10.1039/c7md00278e

APA

Pippione, A. C., Federico, A., Ducime, A., Sainas, S., Boschi, D., Barge, A., ... Lolli, M. L. (2017). 4-Hydroxy-N -[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide: A novel inhibitor of the canonical NF-κB cascade. MedChemComm, 8(9), 1850-1855. https://doi.org/10.1039/c7md00278e

CBE

Pippione AC, Federico A, Ducime A, Sainas S, Boschi D, Barge A, Lupino E, Piccinini M, Kubbutat M, Contreras JM, Morice C, Al-Karadaghi S, Lolli ML. 2017. 4-Hydroxy-N -[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide: A novel inhibitor of the canonical NF-κB cascade. MedChemComm. 8(9):1850-1855. https://doi.org/10.1039/c7md00278e

MLA

Vancouver

Author

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. / 4-Hydroxy-N -[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide: A novel inhibitor of the canonical NF-κB cascade. I: MedChemComm. 2017 ; Vol. 8, Nr. 9. s. 1850-1855.

RIS

TY - JOUR

T1 - 4-Hydroxy-N -[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide: A novel inhibitor of the canonical NF-κB cascade

AU - Pippione, Agnese C.

AU - Federico, Antonella

AU - Ducime, Alex

AU - Sainas, Stefano

AU - Boschi, Donatella

AU - Barge, Alessandro

AU - Lupino, Elisa

AU - Piccinini, Marco

AU - Kubbutat, Michael

AU - Contreras, Jean Marie

AU - Morice, Christophe

AU - Al-Karadaghi, Salam

AU - Lolli, Marco L.

PY - 2017

Y1 - 2017

N2 - 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.

AB - 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.

U2 - 10.1039/c7md00278e

DO - 10.1039/c7md00278e

M3 - Article

VL - 8

SP - 1850

EP - 1855

JO - MedChemComm

JF - MedChemComm

SN - 2040-2511

IS - 9

ER -