4.7 Article

Discovery of novel sesquistilbene indanone analogues as potent anti-inflammatory agents

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 113, Issue -, Pages 63-74

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.02.021

Keywords

Indanone; Anti-inflammatory; TLR4/JNK/NF-kappa B

Funding

  1. National Natural Science Foundation of China [81373276]
  2. Shanghai Municipal Committee of Science and Technology [14XD1400300, 13JC1401200]

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To develop novel anti-inflammatory agents with improved pharmaceutical profiles, twenty-eight novel sesquistilbene indanone analogues were synthesized and evaluated for anti-inflammatory activity using RAW264.7 cells. Among these compounds, compound ilk was found to be one of the most potent analogues in inhibiting NO production in LPS-stimulated RAW264.7 cells. Furthermore, it could also significantly suppress LPS-induced iNOS and COX-2 expression and NO production through TLR4/JNK/NF-kappa B signaling pathway in a concentration dependent manner. (C) 2016 Elsevier Masson SAS. All rights reserved.

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