虎春艳,郑喜,林玉萍,王秀丽,毛泽伟.化学通报,2017,80(4):396-399.
哌嗪取代查尔酮衍生物的合成及其细胞毒活性
Synthesis and cytotoxic activities of piperazine stubstituted chalcone derivatives
投稿时间:2016-07-12  修订日期:2016-09-08
DOI:
中文关键词:  哌嗪  查尔酮衍生物  合成  细胞毒活性
英文关键词:piperazine  chalcone derivatives  synthesis  cytotoxic activities
基金项目:云南省应用基础研究项目(2014FZ087)
作者单位E-mail
虎春艳 云南中医学院中药学院 77461952@qq.com 
郑喜 云南中医学院第一附属医院中心实验室  
林玉萍 云南中医学院中药学院  
王秀丽 云南中医学院中药学院  
毛泽伟* 云南中医学院中药学院 ydmason@163.com 
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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,经羟醛缩合脱水、取代反应生成4-甲氧基-4’-(1-哌嗪基)查尔酮(2)。再通过酰化反应合成了10 个新型含哌嗪的查尔酮衍生物,其结构经1H NMR、13C NMR及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,化合物3e和4d对肿瘤细胞株Hela和A549均表现出较好的细胞毒活性,可做进一步研究。
英文摘要:
      series of chalcone derivatives containing piperazine group have synthesized starting from 4-methoxybenzaldehyde and 2-bromo-4''- fluoroacetophenone by Aldol reaction, dehydration and substitution. Their structures were characterized by 1H NMR, 13C NMR andHRMS. The cytotoxic activities in vitro of the synthesized compounds were evaluated against a panel of human tumor cell lines by the MTT assay. The biological results demonstrated that compound 3e and 4d show good cytotoxic activites against Hela and A549, and could be used as lead compounds for further research.
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