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哌嗪取代查尔酮衍生物的合成及其细胞毒活性
引用本文:虎春艳,郑喜,林玉萍,王秀丽,毛泽伟.哌嗪取代查尔酮衍生物的合成及其细胞毒活性[J].化学通报,2017,80(4):396-399.
作者姓名:虎春艳  郑喜  林玉萍  王秀丽  毛泽伟
作者单位:云南中医学院中药学院,云南中医学院第一附属医院中心实验室,云南中医学院中药学院,云南中医学院中药学院,云南中医学院中药学院
基金项目:云南省应用基础研究项目(2014FZ087)
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。

关 键 词:哌嗪  查尔酮衍生物  合成  细胞毒活性
收稿时间:2016/7/12 0:00:00
修稿时间:2016/9/8 0:00:00

Synthesis and cytotoxic activities of piperazine stubstituted chalcone derivatives
HU Chun-yan,ZHENG Xi,LIN Yu-ping,WANG Xiu-li and MAO Ze-wei.Synthesis and cytotoxic activities of piperazine stubstituted chalcone derivatives[J].Chemistry,2017,80(4):396-399.
Authors:HU Chun-yan  ZHENG Xi  LIN Yu-ping  WANG Xiu-li and MAO Ze-wei
Institution:School of Traditional Chinese Medicine,Yunnan University of Traditional Chinese Medicine;Central laboratory,The NO Affiliated Hospital of Yunnan University of Traditional Chinese Medicine,School of Traditional Chinese Medicine,Yunnan University of Traditional Chinese Medicine;Central laboratory,The NO Affiliated Hospital of Yunnan University of Traditional Chinese Medicine,School of Traditional Chinese Medicine,Yunnan University of Traditional Chinese Medicine;Central laboratory,The NO Affiliated Hospital of Yunnan University of Traditional Chinese Medicine,School of Traditional Chinese Medicine,Yunnan University of Traditional Chinese Medicine;Central laboratory,The NO Affiliated Hospital of Yunnan University of Traditional Chinese Medicine,School of Traditional Chinese Medicine,Yunnan University of Traditional Chinese Medicine;Central laboratory,The NO Affiliated Hospital of Yunnan University of Traditional Chinese Medicine
Abstract: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.
Keywords:piperazine  chalcone derivatives  synthesis  cytotoxic activities
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