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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 and Contreras, Jean Marie, et al. (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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type
Contribution to journal
publication status
published
subject
in
MedChemComm
volume
8
issue
9
pages
6 pages
publisher
Royal Society of Chemistry
external identifiers
  • scopus:85029845664
  • wos:000411437800013
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
2018-08-12 04:39:56
@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},
  volume       = {8},
  year         = {2017},
}