Sammanfattning
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.
Originalspråk | engelska |
---|---|
Sidor (från-till) | 1850-1855 |
Antal sidor | 6 |
Tidskrift | MedChemComm |
Volym | 8 |
Nummer | 9 |
DOI | |
Status | Published - 2017 |
Ämnesklassifikation (UKÄ)
- Läkemedelskemi
- Cancer och onkologi