Reithofer Michael R, Schwarzinger Anne, Valiahdi Seied M, Galanski Mathea S, Jakupec Michael A, Keppler Bernhard K
University of Vienna, Institute of Inorganic Chemistry, Waehringer Strasse 42, A-1090 Vienna, Austria.
J Inorg Biochem. 2008 Dec;102(12):2072-7. doi: 10.1016/j.jinorgbio.2008.07.006. Epub 2008 Jul 23.
(OC-6-33)-Dichlorido(ethane-1,2-diamine)dihydroxidoplatinum(IV) (1) was carboxylated using succinic- or 3-methylglutaric anhydride. The resulting bis(carboxylato)platinum(IV) complexes display free, uncoordinated carboxylic acid groups which were further derivatized with primary aliphatic alcohols. The complexes were characterized in detail by elemental analysis, ESI-MS, FT-IR, as well as multinuclear (1H, 13C, 15N, 195Pt) NMR spectroscopy. Cytotoxic properties were evaluated in four human tumor cell lines originating from ovarian carcinoma (CH1, SK-OV-3), cervical carcinoma (HeLa) and colon carcinoma (SW480) by means of the MTT assay (MTT = 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide). Structure-activity relationships showed that the cytotoxicity increased with increasing lipophilicity of the alcoholate moiety yielding IC50 values in the low micromolar or even low nanomolar range.
（OC-6-33）-二氯（乙烷-1,2-二胺）二羟基铂（IV）（1）用琥珀酸酐或3-甲基戊二酸酐进行羧基化反应。所得的双（羧基）铂（IV）配合物含有游离的、未配位的羧酸基团，这些基团再用伯脂肪醇进一步衍生化。通过元素分析、电喷雾电离质谱（ESI-MS）、傅里叶变换红外光谱（FT-IR）以及多核（1H、13C、15N、195Pt）核磁共振光谱对这些配合物进行了详细表征。通过MTT法（MTT = 3-（4,5-二甲基-2-噻唑基）-2,5-二苯基-2H-四唑溴盐）在源自卵巢癌（CH1、SK-OV-3）、宫颈癌（HeLa）和结肠癌（SW480）的四种人类肿瘤细胞系中评估了细胞毒性特性。构效关系表明，细胞毒性随着醇盐部分亲脂性的增加而增强，半数抑制浓度（IC50）值处于低微摩尔甚至低纳摩尔范围。
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