含靶向性双膦酸基团的乙二胺衍生物的合成及细胞毒活性

Synthesis and Cytotoxicity of Ethylenediamine Derivatives with Bone-targeting Bisphosphonate Groups

设计并合成一类含靶向性双膦酸基团的N,N’-二乙基乙二胺衍生物,通过元素分析、核磁氢谱、碳谱、磷谱、高分辨质谱对所有化合物进行结构表征,并利用CCK-8试剂盒检测化合物对卵巢癌SKOV3及骨肉瘤MG-63细胞系72h的体外抑制活性,并通过SPSS软件计算IC50值,寻找潜在抗肿瘤先导化合物。

A novel series of N,N'-diethylethylenediamine derivatives containing N,N'-dibisphosphonate substituents have been synthesized and characterized by elemental analysis,1H NMR,13 C NMR,31 P NMR and HRMS spectra.The in vitro cytotoxicities of all compounds were tested with CCK-8 by WST-8 assay against SKOV3 and MG-63 cell lines after 72 h incubation and the IC50 values were obtained by SPSS software.