| 高 慧,万春平,朱加洪,夏应娇,张艳娇,毛泽伟.化学通报,2018,81(1):77-82. |
| 含N-烷基哌嗪取代呋喃查尔酮类化合物的合成及其 生物活性评价 |
| Synthesis and biological evaluation of N-alkylpiperazine substituted furanyl chalcone derivatives |
| 投稿时间：2017-07-11 修订日期：2017-07-30 |
| DOI： |
| 中文关键词: 呋喃查尔酮 合成 生物活性评价 |
| 英文关键词:furanyl chalcone synthesis biological evaluation |
| 基金项目:国家自然科学基金项目（81560620）；云南省应用基础研究项目（2014FZ078, 2014FZ087） |
|
| 摘要点击次数: 2323 |
| 全文下载次数: 0 |
| 中文摘要: |
| 为了寻找结构新颖的生物活性分子，采用活性亚结构拼接原理设计合成了12个未见文献报道的新型哌嗪取代呋喃查尔酮衍生物(3a～3l)，其结构经1H NMR、13C NMR和HRMS确证。分别采用MTT法和小鼠巨噬细胞Raw 264.7炎症模型对目标化合物体外细胞毒活性和抗炎活性进行测试，结果表明，哌嗪环上的取代基对化合物的生物活性有明显的影响。特别是化合物3j和3k对肿瘤细胞株Hela和A549均表现出良好的体外抑制活性，而且化合物3d能有效抑制NO的生成，均可作进一步研究。 |
| 英文摘要: |
| With development of new potent biological agents, twelve new 4’-(N-substitued-1-piperazinyl) furanyl chalcone derivatives (3a～3l) have been designed and synthesized by the general principle of molecular hybridization. The structures were characterized by 1H NMR, 13C NMR and HRMS. In vitro cytotoxic activity against a panel of human tumor cell lines (Hela, A549 and SGC7901) by the MTT assay, and anti-inflammatory activity in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages were evaluated. The result indicated that the substituents of the NH group of piperazine ring have an obvious influence on biological activities. Especially, compounds 3j and 3k were found to be the potent compounds against Hela and A549, and compounds 3d had the inhibitory effect on the generation of NO, which are to be lead compounds for further SAR research. |
| 查看全文 查看/发表评论 下载PDF阅读器 |
| 关闭 |