具空间位阻效应的抗肿瘤铂配合物研究现状  

Current Status of Sterically Hindered Antitumor Platinum Complexes

作　　者：丛艳伟[1] 普绍平[1] 朱泽兵 李学杰 彭娟 

机构地区：[1]昆明贵金属研究所,云南昆明650221 [2]昆明贵研药业有限公司,云南昆明650221

出　　处：《药学进展》2007年第4期145-149,共5页Progress in Pharmaceutical Sciences

基　　金：云南省技术创新人才培养项目(2004PY-07)

摘　　要：综述近年来有关具空间位阻效应的单吡啶(氨/胺)类、双吡啶类、双咪唑类、喹啉类抗肿瘤铂配合物的研究与开发,结合若干具代表性的铂配合物探讨其抗肿瘤活性、克服交叉耐药性和作用机制及构效关系。具空间位阻效应的铂配合物是目前铂类抗肿瘤药物研究的一个重要方向,其在结构上和抗癌机制上均不同于顺铂,可部分或完全克服与顺铂的交叉耐药性,具良好的开发前景。The recent research and development of sterically hindered antitumor platinum complexes of the types of mono-pyridine （ammino/amine）, bis-pyridine, bis-imidazol and quinoline were reviewed. The antitumor activities, the mechanisms of action and advoidanee of cross resistance and the structure-activity relationship of these platinum complexes were disoussed based on some representatives. Sterieally hindered platinum complexes have become an important direction of research on antitumor platinum drugs, which differ from eisplatin in structure and antitumor mechanism, avoid the cross resistance with eisplatin partly or completely and have broad development prospects.

关 键 词：空间位阻 铂配合物 抗肿瘤活性 交叉耐药性 作用机制 构效关系 

分 类 号：R730.5[医药卫生—肿瘤]