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4-Hydroxy-N -[3,5-b...
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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- Pippione, Agnese C. (author)
- University of Turin
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- Federico, Antonella (author)
- University of Turin
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- Ducime, Alex (author)
- University of Turin
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- Sainas, Stefano (author)
- University of Turin
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- Boschi, Donatella (author)
- University of Turin
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- Barge, Alessandro (author)
- University of Turin
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- Lupino, Elisa (author)
- University of Turin
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- Piccinini, Marco (author)
- University of Turin
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- Kubbutat, Michael (author)
- ProQinase GmbH
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- Contreras, Jean Marie (author)
- Prestwick Chemical PC SAS
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- Morice, Christophe (author)
- Prestwick Chemical PC SAS
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- Al-Karadaghi, Salam (author)
- Lund University,Lunds universitet,Biokemi och Strukturbiologi,Centrum för Molekylär Proteinvetenskap,Kemiska institutionen,Institutioner vid LTH,Lunds Tekniska Högskola,Biochemistry and Structural Biology,Center for Molecular Protein Science,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH
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- Lolli, Marco L. (author)
- University of Turin
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(creator_code:org_t)
- 2017
- 2017
- English 6 s.
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In: MedChemComm. - : Royal Society of Chemistry (RSC). - 2040-2503 .- 2040-2511. ; 8:9, s. 1850-1855
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Abstract
Subject headings
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- 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.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin -- Cancer och onkologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine -- Cancer and Oncology (hsv//eng)
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- art (subject category)
- ref (subject category)
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- By the author/editor
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Pippione, Agnese ...
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Federico, Antone ...
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Ducime, Alex
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Sainas, Stefano
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Boschi, Donatell ...
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Barge, Alessandr ...
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show more...
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Lupino, Elisa
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Piccinini, Marco
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Kubbutat, Michae ...
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Contreras, Jean ...
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Morice, Christop ...
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Al-Karadaghi, Sa ...
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Lolli, Marco L.
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show less...
- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Medicinal Chemis ...
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Clinical Medicin ...
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and Cancer and Oncol ...
- Articles in the publication
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MedChemComm
- By the university
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Lund University