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Synthesis and biological evaluation of acetylenic chalcones as novel anti-inflammatory agents. 2015
Chengguang Zhao, and
Jianpeng Feng, and
Mingming Zuo, and
Ying Zhang, and
Jianfeng Zhao, and
Shanmei Xu, and
Suqing Zheng, and
Yali Zhang, and
Qinqin Tang, and
Zhongqiu Lu, and
Guang Liang, and
Jianmin Zhou
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.
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