Synthesis and Anti‐Inflammatory Activity of 2‐Amino‐4,5,6,7‐tetrahydrobenzo[ b ]thiophene‐Derived NRF2 Activators

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:	Lipopolysaccharides Kelch-Like ECH-Associated Protein 1 NF-E2-Related Factor 2 Tumor Necrosis Factor-alpha Interleukin-6 NF-kappa B Anti-Inflammatory Agents Thiophenes General Chemistry Dinoprostone Rats Mice Cyclooxygenase 2 Humans Animals Cytokines RNA Messenger Inflammation Mediators
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:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5858605998fcc3df15b9481074bfd558 https://doi.org/10.1002/open.202200181 Zobrazit plný text záznamu Plný text