Autor: |
Kit‐Kay Mak, Zhang Shiming, Ola Epemolu, Albena T. Dinkova‐Kostova, Geoffrey Wells, Irina G. Gazaryan, Raghavendra Sakirolla, Zulkefeli Mohd, Mallikarjuna Rao Pichika |
Rok vydání: |
2022 |
Předmět: |
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Zdroj: |
ChemistryOpen. 11 |
ISSN: |
2191-1363 |
Popis: |
This is the first study investigating the nuclear factor (erythroid-derived 2)-like 2 (NRF2) activity of compounds containing a new scaffold, tetrahydrobenzo[b]thiophene. Eighteen compounds were synthesised and confirmed their NRF2 activation through NQO1 enzymatic activity and mRNA expression of NQO1 and HO-1 in Hepa-1c1c7 cells. The compounds disrupted the interaction between Kelch-like ECH-associated protein 1 (KEAP1) and NRF2 via interfering with the KEAP1's Kelch domain. The compounds exhibited anti-inflammatory activity in Escherichia coli Lipopolysaccharide (LPS |
Databáze: |
OpenAIRE |
Externí odkaz: |
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