有机化学 ›› 2011, Vol. 31 ›› Issue (05): 708-714. 上一篇    下一篇

研究论文

香豆素西佛碱衍生物的合成及抗肿瘤活性研究

王辉1,郑伟华1,谢凤妮1,宋化灿*,2   

  1. (1华南师范大学化学与环境学院 广州 510006)
    (2中山大学化学与化学工程学院 广州 510275)
  • 收稿日期:2010-09-02 修回日期:2010-11-08 发布日期:2010-12-30
  • 通讯作者: 宋化灿 E-mail:yjhxhc@mail.sysu.edu.cn, cedc19@zsu.edu.cn, cesshc@mail.sysu.edu.cn

Synthesis and Biological Evaluation of Coumarin Schiff Base Deriva-tives as Novel Antitumor Inhibitors

Wang Hui1 Zheng Weihua1 Xie Fengni1 Song Huacan*,2   

  1. (1 School of Chemistry and Environment, South China Normal University, Guangzhou 510006)
    (2 School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275)
  • Received:2010-09-02 Revised:2010-11-08 Published:2010-12-30

设计合成了18个未见文献报道的含席夫碱结构的香豆素衍生物, 其结构经1H NMR, 13C NMR, ESI-MS和元素分析确证. 体外对人口腔鳞癌细胞KB及多药耐药株KBv200的初步毒性试验表明, 化合物4a, 4b, 5b, 3d4d具有中等的抗肿瘤活性, 并对其构效关系进行了讨论.

关键词: 香豆素衍生物, 席夫碱, 抗肿瘤活性, KB和KBv200

A series of coumarin Schiff base analogues were synthesized. Their structures were characterized by 1H NMR, 13C NMR, ESI-MS techniques and elemental analysis. Preliminary bioassays for in vitro antitumour activities against KB and KBv200 cells indicated that compounds 4a, 4b, 5b, 3d and 4d exhibited middle potent antitumour activities. The relatives of structure and activity were discussed.

Key words: coumarin derivative, Schiff base, antitumor activity, KB and KBv200