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

[ Vol. 11 , Issue. 6 ]


Chengguang Zhao, Jianpeng Feng, Mingming Zuo, Ying Zhang, Jianfeng Zhao, Shanmei Xu, Suqing Zheng, Yali Zhang, Qinqin Tang, Zhongqiu Lu, Guang Liang and Jianmin Zhou   Pages 567 - 572 ( 6 )


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.


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


Director, Chemical Biology Research Center, College of Pharmaceutical Sciences, Wenzhou Medical University, China.

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