新型双（羧基）二氯二乙胺合铂（IV）配合物的合成与表征，其细胞毒性高于顺铂。
Synthesis and characterization of novel bis(carboxylato)dichloridobis(ethylamine)platinum(IV) complexes with higher cytotoxicity than cisplatin.
机构信息
University of Vienna, Institute of Inorganic Chemistry, Währinger Strasse 42, A-1090 Vienna, Austria.
出版信息
Eur J Med Chem. 2011 Nov;46(11):5456-64. doi: 10.1016/j.ejmech.2011.09.006. Epub 2011 Sep 8.
A series of six novel bis(carboxylato)dichloridobis(ethylamine)platinum(IV) complexes was synthesized and characterized in detail by elemental analysis, FT-IR, ESI-MS, HPLC, multinuclear ((1)H, (13)C, (15)N, (195)Pt) NMR spectroscopy and in one case by X-ray diffraction. Cytotoxic properties of the complexes were evaluated in four human tumor cell lines originating from ovarian carcinoma (CH1 and SK-OV-3), colon carcinoma (SW480) and non-small cell lung cancer (A549) by means of the MTT colorimetrical assay. In addition, their octanol/water partition coefficients (log P values) were determined. Remarkably the most active (and also most lipophilic) compounds, having 4-propyloxy-4-oxobutanoato and 4-(2-propyloxy)-4-oxobutanoato axial ligands, showed IC(50) values down to the low nanomolar range.
合成并详细表征了一系列六种新型双（羧酸根）二氯二（乙胺）合铂（IV）配合物，通过元素分析、FT-IR、ESI-MS、HPLC、多核（^1H、^13C、^15N、^195Pt）NMR 光谱和 X 射线衍射进行了表征。通过 MTT 比色法在源自卵巢癌（CH1 和 SK-OV-3）、结肠癌（SW480）和非小细胞肺癌（A549）的四种人肿瘤细胞系中评估了配合物的细胞毒性。此外，还测定了它们的辛醇/水分配系数（log P 值）。值得注意的是，最具活性（也是最亲脂性）的化合物具有 4-丙氧基-4-氧代丁酸酯和 4-（2-丙氧基）-4-氧代丁酸酯轴向配体，其 IC（50）值低至纳摩尔范围。
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