新型卟啉苦马豆素衍生物的合成及抗肿瘤活性  

Synthesis and Anticancer Activity of Novel Porphyrin-swainsonine Derivatives

作　　者：张志辉[1] 王淑勋 ZHANG Zhihui;WANG Shuxun(Shijiazhuang No.4 Pharmaceutical Co.,Ltd.,Shijiazhaung 052165,China)

机构地区：[1]石家庄四药有限公司,河北石家庄052165

出　　处：《合成化学》2024年第3期232-236,共5页Chinese Journal of Synthetic Chemistry

基　　金：河北省重点研发计划项目(22372705D)。

摘　　要：新型抗肿瘤药的研究越来越受到重视。本文将氨基卟啉或羟基卟啉、POCl_(3)和苦马豆素缩合,合成了7种新型卟啉苦马豆素衍生物(1a~1g),并对其抗肿瘤活性进行了评价。结果表明:设计合成的衍生物1a~1g对SGC-7901和Eca-109肿瘤细胞均具有抑制作用。衍生物1c对SGC-7901和Eca-109细胞的IC_(50)分别为1.77±0.14μM和3.32±0.13μM,抗癌活性明显优于苦马豆素。所有衍生物的结构均经核磁共振、质谱和元素分析表征。New research into anticancer drugs is increasingly gaining attention.In this paper,seven new swainsonine derivatives(1a~1g)were synthesized by the condensation of aminoporphyrin or hydroxyl porphyrin,POCl_(3) and swainsonine,and their antitumor activities were evaluated.The results showed that derivatives 1a~1g all had inhibitory effects on SGC-7901 and Eca-109 tumor cells.The IC_(50) of derivative 1c for SGC-7901 and Eca-109 cells was 1.77±0.14μM and 3.32±0.13μM,respectively,which clearly indicates superior anticancer activity compared to swainsonine.The structures of all derivatives were confirmed by nuclear magnetic resonance,mass spectrometry and elemental analysis.

关 键 词：苦马豆素 卟啉 抗癌活性 卟啉苦马豆素衍生物 合成 

分 类 号：R914[医药卫生—药物化学]