有机化学 ›› 2017, Vol. 37 ›› Issue (1): 237-241.DOI: 10.6023/cjoc201605021 上一篇    下一篇

研究简报

新型4'-(N-取代-1-哌嗪基)查尔酮衍生物的合成及其抗肿瘤活性

林玉萍a, 虎春艳a, 郑喜b, 王秀丽a, 万春平b, 毛泽伟a   

  1. a 云南中医学院中药学院 昆明 650500;
    b 云南中医学院第一附属医院中心实验室 昆明 650021
  • 收稿日期:2016-05-12 修回日期:2016-06-20 出版日期:2017-01-25 发布日期:2016-07-15
  • 通讯作者: 毛泽伟 E-mail:ydmason@163.com
  • 基金资助:

    国家自然科学基金(No. 81460624)和云南省教育厅基金(No. 2014Z119)资助项目.

Synthesis and Anti-tumor Activities of Novel 4'-(N-Substitued-1-piperazinyl) chalcone Derivatives

Lin Yupinga, Hu Chunyana, Zheng Xib, Wang Xiulia, Wan Chunpingb, Mao Zeweia   

  1. a School of Traditional Chinese Medicine, Yunnan University of Traditional Chinese Medicine, Kunming 650500;
    b Central Laboratory, The No. 1 Affiliated Hospital of Yunnan University of Traditional Chinese Medicine, Kunming 650021
  • Received:2016-05-12 Revised:2016-06-20 Online:2017-01-25 Published:2016-07-15
  • Supported by:

    Project supported by theNational Natural Science Foundation of China(No. 81460624) and the Foundation of Yunnan Province Department of Education(No. 2014Z119).

为了寻找活性较高的抗肿瘤新型分子,采用活性亚结构拼接的方法,将查尔酮和哌嗪连接起来,并通过衍生化,设计合成了10个未见文献报道的新型4'-(N-取代-1-哌嗪基)查尔酮衍生物3a~3j,其结构经1H NMR、13C NMR和HRMS确证.采用溴化噻唑蓝四氮唑(MTT)法测试了目标化合物体外抗肿瘤活性(Hela,A549和SGC7901),结果表明化合物3f、3i3j均表现出良好的细胞毒活性,可做进一步研究.

关键词: 查尔酮, 哌嗪, 合成, 抗肿瘤活性

With the aim of developing new potent anticancer agents,a series of novel 4'-(N-substitued-1-piperazinyl) chalcone derivatives 3a~3j have been designed and synthesized based on the structure of the chalcone by molecular hybridization.The structures were characterized by 1H NMR,13C NMR and HRMS.These derivatives were evaluated for their in vitro anti-tumor activity against a panel of human tumor cell lines(Hela,A549 and SGC7901) by the thiazolyl blue tetrazolium bromide(MTT) assay.The result indicated that compounds 3f,3i and 3j were found to be the potent compounds against human tumor cell lines,which are to be lead compounds for further structural modifications and activity research.

Key words: chalcone, piperazine, synthesis, anti-tumor activity