Bis‐ and Tris(carboxylato)platinum(IV) Complexes with Mixed Am(m)ine Ligands in the
<i>trans</i>
Position Exhibiting Exceptionally High Cytotoxicity
作者:Björn R. Hoffmeister、Michaela Hejl、Michael A. Jakupec、Mathea Sophia Galanski、Bernhard K. Keppler
DOI:10.1002/ejic.201403226
日期:2015.4
A series of seven diam(m)inebis(carboxylato)dihydroxidoplatinum(IV) and eleven diam(m)inetris(carboxylato)hydroxidoplatinum(IV) complexes with am(m)ine ligands in the trans position was synthesized and characterized by multinuclear 1H, 13C, 15N, 195Pt NMR spectroscopy. IC50 values for all eighteen substances were determined by means of the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide
合成了一系列具有反位氨基(间)氨酸配体的七个 diam(m)inebis(羧基)二羟基铂(IV)和 11 个 diam(m)inetris(羧基)羟基铂(IV)配合物,并通过多核 1H 表征, 13C、15N、195Pt NMR光谱。所有十八种物质的 IC50 值通过 3-(4,5-二甲基噻唑-2-基)-2,5-二苯基-2H-溴化四唑 (MTT) 测定对三种人类癌细胞系进行测定。在顺铂敏感的 CH1(PA-1) 癌细胞中,diam(m)inebis(carboxylato)dihydroxidoplatinum(IV) 复合物在微摩尔范围内显示出 50% 的抑制浓度,而对于 diam(m)inetris(羧基)氢氧化铂(IV)系列,发现有希望的 IC50 值在纳摩尔范围内。