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有机化学
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有机化学 ›› 2008, Vol. 28 ›› Issue (12): 2095-2101. 上一篇    下一篇

研究论文

二芳醚基哌嗪类衍生物的合成及细胞毒活性研究

阳应华; 张丽娟; 杨雷香; 王晓雨; 巫秀美 ; 赵 昱*   

  1. (浙江大学药学院中药与天然药物研究室 杭州 310058)
  • 收稿日期:2008-02-29 修回日期:2008-06-01 发布日期:2008-12-28
  • 通讯作者: 赵 昱

Synthesis of Diaryl Ether Substituted Piperazine Derivatives and Their Cytotoxic Activities

YANG, Ying-Hua; ZHANG, Li-Juan; YANG, Lei-Xiang; WANG, Xiao-Yu ;
WU, Xiu-Mei ; ZHAO, Yu*
  

  1. (Department of Traditional Chinese Medicine and Natural Drug Research, College of Pharmaceutical Sciences,
    Zhejiang University, Hangzhou 310058)
  • Received:2008-02-29 Revised:2008-06-01 Published:2008-12-28
  • Contact: ZHAO, Yu

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1951

被引次数

8 | 1

根据拼合原理, 设计并合成了21个未见报道的新的二芳醚基哌嗪类衍生物, 其结构用1H NMR, ESI-MS, HRMS进行了确证, 初步生物活性测定实验证明部分目标化合物具有良好的细胞毒活性. 化合物4i分别对人食管癌(Eca109)细胞株和人鼻咽癌(CNE)细胞株的IC50为7.13和4.54 μmol•L－1, 与对照品顺铂(DDP)相近. 化合物5d对人鼻咽癌细胞株也表现较好的活性, 其IC50为8.49 μmol•L－1.

关键词: 哌嗪, 细胞毒活性, 合成, 二芳醚基

Twenty-one new diaryl ether substituted piperazine derivatives were synthesized and their structures were confirmed by 1H NMR, ESI-MS and HRMS data. The preliminary biological activity tests showed that some of the title compounds had good activities. Compound 4i exhibited a potent cytotoxicity against the Eca109 and CNE cell lines with IC50 values of 7.13 and 4.54 μmol•L－1, respectively, which showed the similar activities to the positive control, cisplatin. Compound 5d also possessed an efficient cytotoxicity aganist CNE cell lines with an IC50 value of 8.49 μmol•L－1.