云南化工2024，Vol.51Issue(1)：34-37,4.DOI:10.3969/j.issn.1004-275X.2024.01.08
雷公藤内酯醇乏氧激活前药的合成与结构表征
Synthesis and Characterization of Hypoxia Actived Prodrug of Triptolide
摘要
Abstract
(OBJECTIVE)The hypoxia actived prodrug of triptolide was synthesized,and its structure was confirmed.Additionally,two con-trol compounds Gem1 and Dox1 were prepared.In total,three Hypoxia actived prodrugs were obtained in order to further antitumor study.(METHOD)We used 2-nitroimidazole as the starting material.Subsequently,3-(2-nitro-1H-imidazole-1-yl)propionic acid has been yielded through nucleophilic substitution and hydrolysis.The target compounds,Gem1 and Dox1 were obtained by condensation reaction of 3-(2-nitro-1H-imidazol-1-yl)propionic acid with triptolide,doxorubicin,and gemcitabine,respectively.And their structures were confirmed using 1H-NMR and high-resolution mass spectrometry.(RESULTS)we successfully obtained the target compound and Dox1 and Gem1.(CONCLUSION)the structures of target compound and Dox1 and Gem1 were confirmed by 1H-NMR and high-resolution mass spectrometry.Three hypoxia activated prodrugs were successfully obtained in order to do further antitumor studies.关键词
雷公藤内酯醇/乏氧激活前药/抗肿瘤Key words
triptolide/hypoxia activated prodrug/antitumor分类
医药卫生引用本文复制引用
张冬梅,阙慧卿,李唯..雷公藤内酯醇乏氧激活前药的合成与结构表征[J].云南化工,2024,51(1):34-37,4.基金项目
福建省卫健委青年科研课题(2020QNA022). （2020QNA022）
