Platinum(II) complexes with mono-aminophosphonate ester targeting group that induce apoptosis through G1 cell-cycle arrest: synthesis, crystal structure and antitumour activity.
Platinum(II) complexes with mono-aminophosphonate ester targeting group that induce apoptosis through G1 cell-cycle arrest: synthesis, crystal structure and antitumour activity.
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DOI：
10.1016/j.ejmech.2013.01.055
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发表时间：
2013-05
影响因子：
6.7
通讯作者：
Ke-Bin Huang;Zhenfeng Chen;Yan-cheng Liu;Zhu-Quan Li;Jian-hua Wei;M. Wang;Guo-Hai Zhang;H. Liang-H.
中科院分区：
文献类型：
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作者：
Ke-Bin Huang;Zhenfeng Chen;Yan-cheng Liu;Zhu-Quan Li;Jian-hua Wei;M. Wang;Guo-Hai Zhang;H. Liang-H.
合成了6个新的氨基膦酸单酯铂(II)配合物，并用元素分析、核磁共振氢谱、ESI-MS和单晶X-射线衍射法进行了表征。它们是单核结构。在化合物1-6的所有晶体结构中，铂中心呈近似正方形的平面构型，在有机溶剂和水中都具有良好的溶解性，对MG-63、SK-OV-3和HepG2细胞具有较强的细胞毒性，但对正常人肝细胞HL-7702的细胞毒性较低。与顺铂不同，它们的抗肿瘤活性是通过G1期细胞周期停滞诱导细胞凋亡来实现的。
Six new platinum(II) complexes with mono-aminophosphonate ester were synthesized and characterized by elemental analysis,1H 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.