含双膦酸基团的铂配合物的设计合成及抗肿瘤活性研究  

Synthesis and Antitumor Activity of Platinum-based Complexes with Bisphosphonate Groups

作　　者：孙艳艳[1] 陈蕾[1] 吴希雯 丁倩[1] 

机构地区：[1]苏州科技大学化学生物与材料工程学院,江苏苏州215009

出　　处：《山东化工》2016年第24期1-2,5,共3页Shandong Chemical Industry

基　　金：国家自然科学基金青年项目(21401137);江苏省大学生创新创业训练计划项目(201510332057X)

摘　　要：设计并合成一系列含双膦酸基团的乙二胺衍生物及其铂配合物,通过核磁、质谱及元素分析对化合物进行结构表征,并通过CCK-8法测定其对卵巢癌及骨肉瘤细胞系的体外抗肿瘤活性,筛选出高活性的典型化合物,为后期研究奠定基础。A series of ethylenediamine derivatives containing bifunctional bisphosphonate substituents and their corresponding dichloroplatinum（Ⅱ） complexes have been synthesized and characterized by elemental analysis,^1H NMR, ^31P NMR, and HRMS spectra. All the compounds were tested for their in vitro eytotoxicity by CCK - 8 assay against SKOV3 and MG - 63. It can be found that representative complex 2 with high cytotoxieity has been screened as a potential antitumor agent for subsequent in vivo study.

关 键 词：铂配合物 双膦酸 抗肿瘤 

分 类 号：R943[医药卫生—药剂学] O641.4[医药卫生—药学]