| 虎春艳,郑 喜,林玉萍,王秀丽,毛泽伟.化学通报,2016,79(11):1089-1092. |
| 含N-取代哌嗪片段的查尔酮衍生物的合成及其细胞毒活性 |
| Synthesis and cytotoxic activities of chalcone derivatives bearing N-substituted piperazine moiety |
| 投稿时间：2016-04-24 修订日期：2016-05-07 |
| DOI： |
| 中文关键词: 查尔酮衍生物 合成 细胞毒活性 |
| 英文关键词:chalcone derivatives synthesis cytotoxic activity |
| 基金项目:云南省应用研究项目（2014FZ087） |
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| 中文摘要: |
| 以4-甲氧基苯甲醛与2-溴-4’-氟苯乙酮为原料，经缩合、取代反应后，再与α-溴代酮或α-溴代酯反应，合成得到8个新的查尔酮哌嗪衍生物 (3a～3h)，其结构经1H NMR、13C NMR和HRMS确证。采用MTT法初步测试了目标化合物的体外细胞毒活性，结果表明当哌嗪环上含酮片段取代的化合物对肿瘤细胞株A549和SGC7901均表现出良好的抑制活性，特别是化合物3a (IC50=0.28μM，2.53μM)，可做进一步研究。 |
| 英文摘要: |
| Eight novel chalcone compounds bearing N-substituted piperazine moiety have been synthesized, and their in vitro cytotoxic activities were evaluated against A549 and SGC7901 by the MTT assay. The structures were characterized by 1H NMR, 13C NMR and HRMS. The results showed that compounds bearing ketones showed better anticancer activity. In particular, compound 3a was found to be the most potent compound against A549 and SGC7901 (IC50=0.28μM and 2.53μM, respectively), which is to be lead compound for further research. |
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