title: Synthesis and biological evaluation of acetylenic chalcones as novel anti-inflammatory agents.
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.
authors: Chengguang
authors: C
authors: Zhao
authors: Jianpeng
authors: J
authors: Feng
authors: Mingming
authors: M
authors: Zuo
authors: Ying
authors: Y
authors: Zhang
authors: Jianfeng
authors: J
authors: Zhao
authors: Shanmei
authors: S
authors: Xu
authors: Suqing
authors: S
authors: Zheng
authors: Yali
authors: Y
authors: Zhang
authors: Qinqin
authors: Q
authors: Tang
authors: Zhongqiu
authors: Z
authors: Lu
authors: Director, Chemical Biology Research Center, College of Pharmaceutical Sciences, Wenzhou Medical University, China.. wzmcliangguang@163.com.
authors: Guang
authors: G
authors: Liang
authors: Jianmin
authors: J
authors: Zhou
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D047188:Chalcones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D016207:Cytokines / Q000096:biosynthesis / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D008070:Lipopolysaccharides / Q000494:pharmacology; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D047188:Chalcones; D016207:Cytokines; D008070:Lipopolysaccharides