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  

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

作　　者：贺怀贞[1] 展颖转[1] 张杰[1] 王涛[1] 

机构地区：[1]西安交通大学医学院,西安710061

出　　处：《应用化学》2012年第1期75-79,共5页Chinese Journal of Applied Chemistry

基　　金：国家自然科学基金(30730110;30901839)资助项目

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。Using isovanillin as the starting material, the lactone ring-opened taspine derivative （ compound 8） was obtained via bromination, benzylatiola, 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.

关 键 词：塔斯品碱 香豆素 荧光 抗癌活性 

分 类 号：O621.3[理学—有机化学] TQ450.2[理学—化学]