新型双膦酸衍生物及其铂配合物的合成与生物活性研究

Synthesis and In Vitro Cytotoxicity of Platinum(Ⅱ) Complexes Bearing N,N'-Dibisphosphonate Substituents

设计并合成一类含N,N’-二双膦酸基团的N,N’-二甲基乙二胺衍生物及其铂配合物,通过核磁共振氢谱、高分辨质谱及元素分析对化合物进行结构确证,通过WST-8法研究其对骨肉瘤细胞系48 h和72 h的体外抗肿瘤活性,并总结构效关系,筛选出潜在抗肿瘤先导化合物。

A series of N,N＇-dibisphosphonate substituted ethylenediamine derivatives and their platinum（II） complexes were prepared and characterized by 1H NMR, elemental analysis and HRMS spectra. The cytotoxicity of all compounds was tested by WST-8 assay with CCK-8 against MG-63 cell line after 48 h and 72 h incubation. The promising antitumor agent（complex 2） with high cytotoxicity has been screened out for subsequent in vivo study.