抗肿瘤钌(Ⅱ)药物的研究进展  

Research Progress of Anti-tumor Ru(Ⅱ) Drugs

作　　者：许小芳 杨啟源 廖兰珊 陈振锋[1] XU Xiao-Fang;YANG Qi-Yuan;LIAO Lan-Shan;CHEN Zhen-Feng(State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources,School of Chemistry and Pharmacy of Guangxi Normal University,Guilin,Guangxi,541004)Abstract:Ruthenium(II)compounds have anti-tumor selectivity and)

机构地区：[1]广西师范大学省部共建药用资源化学与药物分子工程国家重点实验室

出　　处：《玉林师范学院学报》2019年第2期2-11,共10页Journal of Yulin Normal University

基　　金：广西研究生教育创新计划项目(YCBZ2018033)

摘　　要：钌(Ⅱ)化合物具有抗肿瘤选择性并可克服铂类药物的耐药性问题,从而使其成为金属药物研究的热点。抗肿瘤钌(Ⅱ/Ⅲ)药物的研究已取得了重要进展:钌的配合物NAMI-A、KP1019和KP1339已进入临床试验阶段,而DW1/2处于临床前研究阶段。构象刚性的有机钌(Ⅱ)配合物DW1/2是一种蛋白激酶抑制剂,这种蛋白激酶抑制剂为抗肿瘤钌(Ⅱ)化合物的设计提供了新思路。本文对抗肿瘤钌(Ⅱ)药物的设计合成、抗肿瘤活性、作用机制和新疗法等进行综述。Ruthenium(Ⅱ) compounds have anti-tumor selectivity and can overcome the resistance of platinum drugs,which makes them become a hot spot in metal-based drug researches.The development of anti-tumor Ru(Ⅱ/Ⅲ) drugs has achieved satisfied results:Ruthenium complexes NAMI-A,KP1019 and KP1339 have entered clinical trials,while DW1/2 is in the pre-clinical stage.The conformational rigid organometallic ruthenium(Ⅱ) complex DW1/2 is a protein kinase inhibitor,which provides a new idea for the design of anti-tumor Ru(Ⅱ) compounds.This paper summarizes the development of anti-tumor Ru(Ⅱ) drugs,their activities,action mechanism and new therapeutic approaches.

关 键 词：钌(Ⅱ)化合物 抗肿瘤药物 新疗法 

分 类 号：R730[医药卫生—肿瘤] R979.1[医药卫生—临床医学]