非喜树碱类DNA拓扑异构酶Ⅰ抑制剂的研究进展  

Recent Advances in Non-camptothecin DNA Topoisomerase I Inhibitors as Anticancer Drugs

作　　者：孙远[1] 王华萍[1] 周游[1] 尤启冬[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》2011年第9期385-395,共11页Progress in Pharmaceutical Sciences

基　　金："重大新药创制"国家科技重大专项课题(No.2009ZX09501-003)

摘　　要：DNA拓扑异构酶Ⅰ(TopoⅠ)是抗肿瘤治疗的重要靶点。喜树碱类TopoⅠ抑制剂已在肿瘤的临床治疗中被广泛使用,但受分子骨架制约,其存在水溶性低、稳定性差、毒副作用大等缺点,而具有新颖结构的非喜树碱类TopoⅠ抑制剂则有望克服这些缺点。按结构分类综述非喜树碱类TopoⅠ抑制剂的抗肿瘤活性及构效关系研究新进展。DNA Topoisomerase I（Topo I） is a promising and important target for cancer therapy.Camptothecin derivatives as Topo I inhibitors have been widely used to treat tumors in clinic.However,due to some defects of molecular scaffold,camptothecin derivatives have commonly shown poor aqueous-solubility,instability and high toxicity.Developing non-camptothecins as Topo I inhibitors with new scaffold can be expected to overcome these shortcomings.The recent advances in study on the anti-tumor activities and structure-activity relationship of non-camtothecins as Topo I inhibitors were reviewed classifiedly based on their structure characteristics.

关 键 词：拓扑异构酶Ⅰ抑制剂 非喜树碱类化合物 抗肿瘤活性 构效关系 

分 类 号：R96[医药卫生—药理学]