School of Chemistry of Nankai University, Tianjin 300071, PR China.
Eur J Med Chem. 2013 May;63:76-84. doi: 10.1016/j.ejmech.2013.01.055. Epub 2013 Feb 9.
Six new platinum(II) complexes with mono-aminophosphonate ester were synthesized and characterized by elemental analysis, (1)H NMR, ESI-MS as well as single crystal X-ray diffraction analysis. They are mononuclear structures. In all the crystal structures of complexes 1-6, the platinum centre adopts an approximately square-planar geometry, which were found to possess excellent solubility in both organic solvents and water and exhibit considerable cytotoxicity against MG-63, SK-OV-3 and HepG2 cell lines, but low cytotoxicity towards normal human liver cell HL-7702. In contrast to cisplatin, their antitumour activities are achieved through the induction of cell apoptosis by G1 cell-cycle arrest.
六种新型单膦酸酯铂(II)配合物被合成并通过元素分析、(1)H NMR、ESI-MS 以及单晶 X 射线衍射分析进行了表征。它们均为单核结构。在配合物 1-6 的所有晶体结构中,铂中心采用近似的平面四方几何构型,具有良好的有机溶剂和水中的溶解性,对 MG-63、SK-OV-3 和 HepG2 细胞系表现出相当的细胞毒性,但对正常人类肝细胞 HL-7702 的细胞毒性较低。与顺铂不同,它们通过 G1 细胞周期阻滞诱导细胞凋亡来实现抗肿瘤活性。