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

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.