铂类抗肿瘤药物的研究现状  

Current Status of Antitumor Coordination Compounds of Platinum

作　　者：王伸勇[1] 张荣久[2] 张奕华[1] 沈宏[2] 

机构地区：[1]中国药科大学新药研究中心,江苏南京210009 [2]江苏吴中苏药医药开发有限责任公司,江苏南京210009

出　　处：《药学进展》2004年第6期253-257,共5页Progress in Pharmaceutical Sciences

摘　　要：自从顺铂作为第一代抗肿瘤药物被开发利用以来 ,人们一直在寻找广谱、高活性、低毒性和无交叉耐药性的铂类抗肿瘤药物 ,合成和筛选出各种铂络合物。分别介绍根据不同设计思路合成的四价铂络合物、具有活性配体的铂络合物、生物载体为配体的靶向铂络合物、反式铂络合物和具有立体位阻效应的铂络合物及其抗肿瘤活性 ,综述当前铂类抗肿瘤药物的研究现状。Since the discovery of the activity of cisplatin,one of the first generation anticancer drugs,platinum(Pt) drugs which have broader anticancer spectrum,higher activity and less toxicity, but have no cross resistance have been in development. Many new Pt complexes have been synthesized and evaluated for their antitumor activity. Octahedra Pt(IV) complexes,tumor-targeting Pt complexes with biologically active carrier ligands,trans Pt complexes,Pt complexes with steric hindrance and their antitumor activity were introduced. The current status of antitumor coordination compounds of platinum is reviewed.

关 键 词：铂络合物 配体 离去基团 毒性 耐药性 抗肿瘤活性 

分 类 号：R979.1[医药卫生—药品]