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Updated: Apr 17, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and biological evaluation of acetylenic chalcones as novel anti-inflammatory agents
Chengguang Zhao, Jianpeng Feng, Mingming Zuo
1Director, Chemical Biology Research Center, College of Pharmaceutical Sciences, Wenzhou Medical University, China.. wzmcliangguang@163.com.
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.
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