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有机化学
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有机化学 ›› 2004, Vol. 24 ›› Issue (11): 1444-1447. 上一篇    下一篇

研究简报

N-酰基-N'-茄呢基哌嗪衍生物的合成及生物活性

王超杰*, 宋金勇, 赵瑾   

  1. 河南大学化学化工学院 开封 475001
  • 收稿日期:2004-02-09 修回日期:2004-04-24 接受日期:2004-05-17 发布日期:2022-09-21
  • 通讯作者: * E-mail: wcjsxq@henu.edu.cn
  • 基金资助:
    河南省科技厅(Nos. 0323024000, 0311020900)和河南大学重点学科资助项目.

Synthesis and Biological Evaluation of the N-Acyl-N'- solanesylpiperazine Derivatives

WANG Chao-Jie*, SONG Jin-Yong, ZHAO Jin   

  1. College of Chemistry and Chemical Engineering, Henan University, Kaifeng 475001
  • Received:2004-02-09 Revised:2004-04-24 Accepted:2004-05-17 Published:2022-09-21

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以茄呢醇为起始原料和茄呢基哌嗪为关键中间体合成了4个N-酰基-N'-茄呢基哌嗪(4a～4d),以及2个含葡萄糖单元的N-(2-全乙酰葡萄糖基苯甲酰基)-N'-茄呢基哌嗪(5)和N-(2-葡萄糖基苯甲酰基)-N'-茄呢基哌嗪(6),共6个新茄呢基哌嗪衍生物.其结构经元素分析,IR, 1H NMR和MS确证.测试了化合物4c, 5,6对三种人癌细胞(Bel-7402, KB, HCT-8)的体外生理活性,初步结果表明化合物6比4c和5对三种所测细胞有更好的抑制效果.

关键词: 茄呢基哌嗪, N-酰基-N'-茄呢基哌嗪, 合成, 生物活性

Using solanesol as the starting material and N-solanesylpiperazine as the key intermediate, several N-acyl-N'-solanesylpiperazine derivatives (4a～4d) and two similar compounds containing glucosyl fragments, N-(2-acetyl glucosylbenzoyl)-N'-solanesylpiperazine (5) and N-(2-glucosylbenzoyl)-N'-solanesyl piperazine (6), were firstly designed and synthesized to evaluate their biological property. Thestructure of these compounds was confirmed by IR, 1H NMR, MS spectra and elemental analysis. Compounds 4c, 5, 6 were tested in vitro for their anti-tumor activity on KB, Bel-7402 and HCT-8 cells. The preliminary biological studies showed that compound 6 had better inhibition effect than 4c and 5 on the tested three cell lines.

Key words: solanesylpiperazine, N-acyl-N'-solanesylpiperazine, synthesis, bioactivity