喜树碱类药物关键中间体三环羟内酯的合成研究进展  

Progress in synthesis of tricyclic hydroxylactone,a key intermediate of camptothecin drugs

作　　者：王哲 焦晓臻 谢平 WANG Zhe;JIAO Xiao-zhen;XIE Ping(State Key Laboratory of Bioactive Substances and Functions of Natural Medicines,Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation,Institute of MateriaMedica,Chinese Academy of Medical Sciencesand Peking Union Medical College,Beijing 100050)

机构地区：[1]中国医学科学院/北京协和医学院药物研究所天然药物活性物质与功能国家重点实验室活性物质发现与适药化研究北京市重点实验室,北京100050

出　　处：《中国药物化学杂志》2021年第8期618-631,共14页Chinese Journal of Medicinal Chemistry

基　　金：中国医学科学院医学与健康科技创新工程项目(2016-I2M-3-009);中国医学科学院/北京协和医学院中央级公益性科研院所基本科研业务费资助项目(2016ZX350024)。

摘　　要：喜树碱(camptothecin,CPT)为喹啉类生物碱,是一种具有较强细胞毒性的天然抗肿瘤药物,对多种恶性肿瘤有较好的疗效。其作用机制在于能抑制DNA拓扑异构酶I(TOPO I),从而抑制DNA复制、转录等过程,最终导致DNA的断裂。喜树碱类药物为喜树碱衍生物,三环羟内酯为合成喜树碱类药物的通用关键中间体,因此该中间体合成备受关注。本文作者对合成喜树碱类药物的关键中间体三环羟内酯的合成进展作一综述。Camptothecin,a quinoline alkaloid,is a natural anticancer drug w ith strong cytotoxicity and has good curative effect on many kinds of malignant tumors.It can inhibit DNA topoisomerase I (TOPOI) and thus inhibit DNA replication,transcription and other processes,resulting in DNA breakage.The synthesis of the tricyclichydroxylactone has draw n much attention because it is a general key intermediate for the synthesis of camptothecinanalogs.This paper briefly review s the progress in the synthesis of tricyclic hydroxylactone.

关 键 词：喜树碱 DNA拓扑异构酶I 三环羟内酯 通用关键中间体 

分 类 号：R914[医药卫生—药物化学]