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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