4-Hydroxy-N -[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide: A novel inhibitor of the canonical NF-κB cascade
(2017) In MedChemComm 8(9). p.1850-1855- 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.
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- author
- organization
- publishing date
- 2017
- type
- Contribution to journal
- publication status
- published
- subject
- in
- MedChemComm
- volume
- 8
- issue
- 9
- pages
- 6 pages
- publisher
- Royal Society of Chemistry
- external identifiers
-
- wos:000411437800013
- pmid:30108896
- scopus:85029845664
- ISSN
- 2040-2503
- DOI
- 10.1039/c7md00278e
- language
- English
- LU publication?
- yes
- id
- 585b1a46-12b4-464e-a2bc-3810d800a245
- date added to LUP
- 2017-10-10 08:00:06
- date last changed
- 2024-08-05 06:05:58
@article{585b1a46-12b4-464e-a2bc-3810d800a245, abstract = {{<p>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.</p>}}, author = {{Pippione, Agnese C. and Federico, Antonella and Ducime, Alex and Sainas, Stefano and Boschi, Donatella and Barge, Alessandro and Lupino, Elisa and Piccinini, Marco and Kubbutat, Michael and Contreras, Jean Marie and Morice, Christophe and Al-Karadaghi, Salam and Lolli, Marco L.}}, issn = {{2040-2503}}, language = {{eng}}, number = {{9}}, pages = {{1850--1855}}, publisher = {{Royal Society of Chemistry}}, series = {{MedChemComm}}, title = {{4-Hydroxy-N -[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide: A novel inhibitor of the canonical NF-κB cascade}}, url = {{http://dx.doi.org/10.1039/c7md00278e}}, doi = {{10.1039/c7md00278e}}, volume = {{8}}, year = {{2017}}, }