有机化学 ›› 2013, Vol. 33 ›› Issue (9): 1988-1993.DOI: 10.6023/cjoc201304028 上一篇    下一篇

研究简报

N-亚苄基橙皮素腙及类似物的合成与细胞活性

刘志平a,b, 韦万兴a, 甘春芳b, 黄燕敏b, 刘盛a, 周敏a, 崔建国b   

  1. a 广西大学化学化工学院 南宁 530004;
    b 广西师范学院化学与生命科学学院 南宁 530001
  • 收稿日期:2013-04-18 修回日期:2013-05-22 发布日期:2013-05-31
  • 通讯作者: 韦万兴 E-mail:chewxwei@yahoo.com.cn
  • 基金资助:

    国家自然科学基金(No. 81060261);广西科学自然科学基金重点(No. 2011jjD20002)资助项目

Synthesis and Cytotoxicity of N-Benzylidene Hesperitin Hydrazones and Analogues

Liu Zhipinga,b, Wei Wanxinga, Gan Chunfangb, Huang Yanminb, Liu Shenga, Zhou Mina, Cui Jianguob   

  1. a College of Chemistry and Chemical Engineer, Guangxi University, Nanning 530004;
    b College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001
  • Received:2013-04-18 Revised:2013-05-22 Published:2013-05-31
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 81060261) and the Natural Science Foundation of Guangxi Province (No. 2011jjD20002)

以天然橙皮素(1)为原料, 与水合肼反应得到了橙皮素腙(2). 2分别与各种取代的芳香醛反应首次合成了8个N-亚苄基橙皮素腙310及6个类似物1116. 所合成产物通过NMR, IR, HR-ESI-MS方法进行了结构确证. MTT(噻唑蓝)蛋白染色法体外抑制肿瘤增值活性测试发现化合物5, 7, 10, 16对胃癌细胞SGC-7901有显著的抑制活性.

关键词: 橙皮素, 橙皮素腙, N-亚苄基, 细胞活性

Hesperitin hydrazone (2) was generated by the reaction of natural hesperitin (1) as raw material with hydrazine hydrate. Eight N-benzylidene hesperitin hydrazones 310 and six analogues 1116 were synthesized by the reaction of 2 with various aldehydes, respectively. The structures of all reaction products were confirmed by NMR, IR and HR-MS techniques. And the cytotoxity against human cancer cell SGC-7901 of the synthesized compounds was also evaluated. The results showed 5, 7, 10 and 16 exhibiting distinct cytotoxity against SGC-7901.

Key words: hesperitin, hesperitin hydrazones, N-benzylidene, cytotoxicity