抗肿瘤双膦酸衍生物的合成及生物活性研究

Synthesis and Biological Activity of 1,3-propanediamine Derivatives with Bisphosphonate Groups

设计并合成一类含功能性双膦酸基团的丙二胺衍生物,通过核磁、高分辨质谱及元素分析等对所有化合物进行结构表征,并通过以WST-8法为原理的CCK-8试剂盒检测对卵巢癌及骨肉瘤细胞系的体外细胞毒活性,得出其IC_(50)值,为筛选潜在化学实体奠定基础。

A series of 1,3 -propanediamine derivatives containing bifunctional bisphosphonate substituents have been synthesized and characterized by elemental analysis, 1H NMR, 13C NMR, 31p 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, indicating that the compounds showed higher cytotoxicity against SKOV3 than that against MG- 63.