抗癌药物喜树碱类衍生物的结构修饰研究进展  

Research Progress on Structural Modification of Camptothecin Derivatives as Anticancer Drug

作　　者：黄楷迪 高苏亚[1] 刘珂珂 汪亚兰 曹甜 王佳 王睿 HUANG Kai-di, GAO Su-ya, LIU Ke-ke, WANG Ya-lan, CAO Tian, WANG Jia, WANG Rui(School Pharmacy, Xi’an Medical University, Shaanxi Xi’an 710021, Chin)

机构地区：[1]西安医学院药学院,陕西西安710021

出　　处：《广州化工》2018年第15期17-18,26,共3页GuangZhou Chemical Industry

基　　金：西安医学院大学生创新项目(2015DXS1-23;2017DC-27;2017DC-82);西安医学院重点建设学科(2016YXXK19);陕西省大学生创新训练项目(2334;2280)

摘　　要：喜树碱是一种重要的天然抗肿瘤药物,但水溶性差、毒副作用较强及容易代谢失活等缺点限制了其作为临床抗肿瘤药物的应用。研究人员对其7、9、10和20位碳进行结构改造,可克服上述缺点。因此,对喜树碱进行结构修饰,仍然是发现临床候选抗癌药物的有效手段。本文对其结构修饰的研究进展进行简要综述,为此类药物的进一步开发提供参考。Camptothecin is an important antitumor product from Camptotheca acuminate. However, thedisadvantages, such as poor solubility, toxicity and metabolic inactivation, have blocked its application as antineoplasticagent. Over the past few decades, the modification of camptothecin at 7-, 9-, 10-and 20-carbon has been carried out bynumerous researchers to conquer its drawbacks. And many excellent camptothecin derivatives have been developed. So bystructural modification of camptothecin, it is still an efficient mean of finding potential anticancer agents. The researchprogress on the development of camptothecin derivatives was briefly reviewed, so as to provide reference for furtherdevelopment of such drugs.

关 键 词：喜树碱 衍生物 结构修饰 

分 类 号：R917[医药卫生—药物分析学]