鬼臼毒素衍生物的构效关系分析及相关新药的研发思路  

Study on Structure-Activity Relationship of Podophyllotoxin Derivatives and Ideas for the Development of Related New Drugs

作　　者：张仕金[1] 朱雄[2] 徐云根[1] 

机构地区：[1]中国药科大学药物化学教研室,江苏南京210009 [2]中国药科大学医药化工研究所,江苏南京210009

出　　处：《药学进展》2012年第11期494-500,共7页Progress in Pharmaceutical Sciences

摘　　要：鬼臼毒素具有良好的抗肿瘤活性,但其水溶性差且毒副作用明显,使其临床应用受到限制。为降低毒性、提高疗效,国内外研究人员对鬼臼毒素进行了结构修饰,合成了大量具有抗肿瘤活性的鬼臼毒素类衍生物。综述近年来鬼臼毒素类化合物的结构修饰、药理活性及构效关系的研究进展。Podophyllotoxin is one of the representative antitumor natural products, but the poor water solubility and significant side effects limit its clinical usage. A series of derivatives of podophyllotoxin based on structure modification were synthesized so as to lower its toxic side effects. This paper surveys the progress in structural modifications, pharmacological activities and structure-activity relationship of podophyllotoxins.

关 键 词：鬼臼毒素 依托泊苷 结构修饰 抗肿瘤 构效关系 

分 类 号：R914[医药卫生—药物化学]