Institut des Sciences et Ingénierie Chimiques, Ecole Polytechnique Fédérale de Lausanne (EPFL) , CH-1015 Lausanne, Switzerland.
Inorg Chem. 2017 Aug 21;56(16):9617-9633. doi: 10.1021/acs.inorgchem.7b01082. Epub 2017 Jul 31.
Dinuclear metal complexes have emerged as a promising class of anticancer compounds with the ability to cross-link biomolecular targets. Here, we describe two novel series of phosphine-linked dinuclear ruthenium(II) p-cymene and gold(I) complexes, in which the length of the connecting poly(ethylene glycol) chain has been systematically modified. The impact of the multinuclearity, lipophilicity, and linker length on the antiproliferative activity of the compounds on tumorigenic (A2780 and A2780cisR) and nontumorigenic (HEK-293) cell lines was assessed. The dinuclear ruthenium(II) complexes were considerably more cytotoxic than their mononuclear counterparts, and a correlation between the lipophilicity of the linker and the cytotoxicity was observed, whereas the cytotoxicity of the gold(I) series is independent of these factors.
双核金属配合物已成为一类很有前途的抗癌化合物，它们能够交联生物分子靶标。在这里，我们描述了两个新系列的膦键连接的双核钌（II）对异丙基苯和金（I）配合物，其中连接的聚（乙二醇）链的长度已被系统地修饰。多核性、亲脂性和连接子长度对化合物在致瘤（A2780 和 A2780cisR）和非致瘤（HEK-293）细胞系中的增殖活性的影响进行了评估。双核钌（II）配合物比单核类似物的细胞毒性大得多，并且观察到连接子的亲脂性与细胞毒性之间存在相关性，而金（I）系列的细胞毒性与这些因素无关。
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