Synthesis and Biological Evaluation of Acetylenic Chalcones as Novel Anti-Inflammatory Agents

Author(s): Chengguang Zhao, Jianpeng Feng, Mingming Zuo, Ying Zhang, Jianfeng Zhao, Shanmei Xu, Suqing Zheng, Yali Zhang, Qinqin Tang, Zhongqiu Lu, Guang Liang, Jianmin Zhou.

Journal Name: Medicinal Chemistry

Volume 11 , Issue 6 , 2015

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Abstract:

37 acetylenic chalcones were designed, synthesized by the Pd/Cu catalyzed Sonogashira coupling reaction, and evaluated for anti-inflammatory activities. A majority of these compounds showed remarkable inhibitions of the expression of inflammatory cytokines in LPS-stimulated macrophages. Six of them demonstrated the dose-dependent inhibition of inflammatory cytokines, and 4f is the most potent antiinflammatory compound. Our results suggest that these active acetylenic chalcones could be further developed as promising candidates for the treatment of inflammatory diseases.

Keywords: Acetylenic chalcones, sonogashira coupling reaction, anti-inflammation, cytokines.

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Article Details

VOLUME: 11
ISSUE: 6
Year: 2015
Page: [567 - 572]
Pages: 6
DOI: 10.2174/1573406411666150209122749
Price: $58

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