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

作者：Tang, Mei-Lin; Zhong, Chen; Liu, Zheng-Yu; Peng, Peng; Liu, Xin-Hua^*; Sun, Xun^*

来源：European Journal of Medicinal Chemistry, 2016, 113: 63-74.

DOI：10.1016/j.ejmech.2016.02.021

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

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.

• 出版日期2016-5-4
• 单位复旦大学