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- Title
Study of the inhibitory effects on TNF-α-induced NF-κB activation of IMD0354 analogs.
- Authors
Li, Yi‐Rong; Lin, Chi‐Chen; Huang, Chih‐Yuan; Wong, Yung‐Hao; Hsieh, Cheng‐Hung; Wu, Han‐Wei; Chen, Jeremy J. W.; Wu, Yu‐Shan
- Abstract
Nuclear factor-κB ( NF-κB) is an important nuclear transcription factor which regulates pro-inflammatory cytokines such as TNF-α, IL-6. Its role as immunoregulatory mediator makes it an attractive target in the development of treatments for inflammatory and autoimmune diseases. In this study, we synthesized derivatives of IMD0354, a known inhibitor for NF-κB, in attempt to understand the effect of benzanilide substitutions on its activity. The inhibition of these analogs on NF-κB activation was analyzed by luciferase assay. The inhibition of IKKβ phosphorylation and pro-inflammatory cytokines was determined by Western blot and real-time PCR. The structure activity relationships showed that the hydroxyl group on IMD0354 is a critical moiety that resulting in the inhibition of NF-κB. Derivatives 1m, 2b, and 2c were shown to inhibit pro-inflammatory cytokine production at low concentration. These newly synthesized compounds may be useful for the treatment of chronic inflammatory disorders or for cancer prevention.
- Subjects
TUMOR necrosis factors; INSULIN derivatives; PHYSIOLOGICAL effects of cytokines; GENETIC transcription; CHRONIC disease treatment; THERAPEUTICS
- Publication
Chemical Biology & Drug Design, 2017, Vol 90, Issue 6, p1307
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.13032