拓扑异构酶I抑制剂研究进展  

Advances in the Researches on Topoisomerase I Inhibitors

作　　者：刘潇[1] 王汝冰 符伟[1] 李志裕[1] 

机构地区：[1]中国药科大学药物化学教研室,江苏南京210009

出　　处：《药学进展》2009年第7期311-320,共10页Progress in Pharmaceutical Sciences

摘　　要：综述近年来拓扑异构酶I抑制剂的研究进展,分类介绍其抗肿瘤活性以及构效关系,并分析讨论其与靶酶结合作用的特点,旨在为设计、合成与筛选新型拓扑异构酶I抑制剂候选化合物提供一定参考。DNA拓扑异构酶I是抗肿瘤药的重要靶点,随着对酶的构象及其抑制剂的深入研究,多种高效低毒的化合物被相继发现并进入临床研究阶段,为肿瘤患者带来了希望。The advances in researches on topoisomerase Ⅰ （topo Ⅰ） inhibitors were introduced, and the species, anticancer activities and their structure-activity relationships （SARs） were summarized. We also analyzed the correlativity between the crystal structure of the ternary complex and their SARs, in order to offer reference for designing, synthesizing and screening new topo Ⅰ inhitibor candidates. The topo Ⅰ has become a useful therapeutic target against cancer, and with the incessant discovery into the conformation of topoisomerase and the related inhitibors, many kinds of compounds with high-eflqciency and low toxicity were discovered. Moreover, some compounds have already entered into the clinical research successfully, which has brought hope for cancer patients.

关 键 词：拓扑异构酶I抑制剂 抗肿瘤药 喜树碱 吲哚并咔唑 茚并异喹啉酮 

分 类 号：R979.1[医药卫生—药品] R914.2[医药卫生—药学]