抗多药耐药紫杉烷类抗肿瘤药物研究进展  

Progress in the Study of Taxanes against Multi-Drug Resistant Tumor

作　　者：于跃[1] 王军飞[1] 王长云[1] 李英霞[2] 

机构地区：[1]中国海洋大学医药学院海洋药物教育部重点实验室,山东青岛266003 [2]复旦大学药学院,上海201203

出　　处：《中国现代应用药学》2012年第1期16-23,共8页Chinese Journal of Modern Applied Pharmacy

基　　金：国家自然科学基金资助项目(81072525)

摘　　要：目的介绍紫杉烷类活性分子与多药耐药肿瘤的构效关系及其临床研究进展。方法综述了近年来国内外相关报道,对紫杉醇6大区域的相关改造分别进行讨论,并就其临床研究及开发上市状况进行概述。结果发现了许多对敏感肿瘤和多药耐药肿瘤抑制活性相当的紫杉烷类药物候选分子。结论熟悉紫杉烷类活性分子与多药耐药肿瘤的构效关系,对开发新一代紫杉烷类抗肿瘤药物具有深远意义。OBJECTIVE To introduce the structure activity relationships （SAR） of taxanes toward multi-drug resistant tumors and progress on its clinical research. METHODS According to the correlative reports in recent years, both the modifications of taxanes and advances in the development of taxane candidates that either have potential for, or are already in, clinical use are reviewed. RESULTS A number of taxanes exhibiting virtually no difference in potency against the drug-sensitive and drug-resistant cell lines were discovered. CONCLUSION It is essential to grasp the SAR of taxanes against drug-resistant tumors and there is far-reaching significance for the discovery of new generation taxane anticancer agents.

关 键 词：紫杉烷 多药耐药 抗肿瘤 

分 类 号：R979.1[医药卫生—药品]