Bernhardt G, Müller R, Gust R, Reile H, Keller C, Spruss T, Schönenberger H
Institut für Pharmazie, Lehrstuhl Pharmazeutische Chemie II, Universität Regensburg, Germany.
Arch Pharm (Weinheim). 1992 Feb;325(2):93-9. doi: 10.1002/ardp.19923250208.
The diastereoisomeric dichloro-[1-(2-, 3- and 4-hydroxyphenyl)-2-phenylethylenediamine]platinum(II) complexes were tested on two human ovarian cancer cell lines NIH: OVCAR-3 and SK-OV-3, both resistant against cisplatin. Dichloro-[threo-1-(3-hydroxyphenyl)-2-phenylethylenediamine]platinum(II) (threo-5-PtCl2) proved to be the most active representative of the new series, producing cytocidal effects at a concentration range of 2.5 to 5.0 microM on the NIH: OVCAR-3 cell line. On the more resistant SK-OV-3 cell line, threo-5-PtCl2 was only moderately active, while in combination with BSO, a GSH level lowering compound, threo-5-PtCl2 showed a strong synergistic effect.
非对映异构的二氯-[1-(2-、3-和4-羟基苯基)-2-苯基乙二胺]铂(II)配合物在两种人卵巢癌细胞系NIH:OVCAR-3和SK-OV-3上进行了测试，这两种细胞系均对顺铂耐药。二氯-[苏式-1-(3-羟基苯基)-2-苯基乙二胺]铂(II)(苏式-5-PtCl2)被证明是新系列中最具活性的代表物，在2.5至5.0微摩尔的浓度范围内对NIH:OVCAR-3细胞系产生杀细胞作用。在更具耐药性的SK-OV-3细胞系上，苏式-5-PtCl2活性一般，而与降低谷胱甘肽水平的化合物BSO联合使用时，苏式-5-PtCl2显示出强烈的协同效应。
