哌嗪取代查尔酮衍生物的合成及其细胞毒活性  

Syntheses and Cytotoxic Activities of Piperazine Substituted Chalcone Derivatives

作　　者：虎春艳[1] 郑喜[2] 林玉萍[1] 王秀丽[1] 毛泽伟[1] 

机构地区：[1]云南中医学院中药学院,昆明650500 [2]云南中医学院第一附属医院中心实验室,昆明650021

出　　处：《化学通报》2017年第4期396-399,共4页Chemistry

基　　金：云南省应用基础研究项目(2014FZ087)资助

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、^(13)C 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。A series of ehalcone derivatives containing piperazine group have been synthesized starting from 4- methoxybenzaldehyde and 2-bromo-4＇- fluoroacetophenone by Aldol reaction, dehydration and substitution. Their struetures were characterized by I H NMR, J3C NMR and HRMS. The cytotoxie activities in vitro of the synthesized compounds were evaluated against a panel of human tumor cell lines by the MTT assay. The biological resulls demonstrated that compound 3e and 4d show good cytotoxic activities against Hela and A549, and could be used as lead compounds for further research.

关 键 词：哌嗪 查尔酮衍生物 合成 细胞毒活性 

分 类 号：TQ460.1[化学工程—制药化工]