应用化学

• 研究论文 • 上一篇    下一篇

内酯开环塔斯品碱香豆素酯衍生荧光化合物的合成及其抗癌活性

贺怀贞*,展颖转,张杰,王涛   

  1. (西安交通大学医学院 西安 710061)
  • 收稿日期:2011-02-21 修回日期:2011-03-30 出版日期:2012-01-10 发布日期:2012-01-10
  • 通讯作者: 贺怀贞,讲师; Tel:029-82657740; Fax:029-82655451; E-mail:hehuaizhen@mail.xjtu.edu.cn; 研究方向:生物荧光探针的合成
  • 基金资助:
    国家自然科学基金(30730110,30901839)资助项目

Synthesis and Anti-tumor Activities of Lactone Ring-Opened Taspine Coumarin Ester Fluorescent Derivatives

HE Huaizhen*, ZHAN Yingzhuan, ZHANG Jie, WANG Tao   

  1. (School of Medicine,Xi′an Jiaotong University,Xi′an 710061)
  • Received:2011-02-21 Revised:2011-03-30 Published:2012-01-10 Online:2012-01-10

摘要:

以异香草醛为原料,经溴代、苄基保护、氧化、Ulmman反应和还原等6步反应合成了塔斯品碱内酯开环衍生物(化合物8)。 通过在其结构中分别引入含有2种不同取代基的香豆素衍生物,设计、合成了2个新型荧光性的内酯开环塔斯品碱香豆素酯衍生物(化合物9a和9b)。  产物结构经IR、1H NMR和MS进行了表征。 同时,对产物的荧光特性及其对乳腺肿瘤细胞增殖的抑制活性进行了初步测定。

关键词: 塔斯品碱, 香豆素, 荧光, 抗癌活性

Abstract:

Using isovanillin as the starting material, the lactone ring-opened taspine derivative(compound 8) was obtained via bromination, benzylation, oxidation, Ulmman reaction and catalytic hydrogenation. Based on this, we designed and synthesized two novel lactone ring-opened taspine coumarin ester fluorescent derivatives with substituted coumarin(compounds 9a and 9b). The structures of the target compounds were characterized by means of IR, 1H NMR and MS. The fluorescence and the anti-tumor activities of the target compounds were preliminarily examined.

Key words: taspine, coumarin, fluorescence, anti-tumor activity

中图分类号: