Synthesis of dinuclear oxadiazole-adamantane platinum(II) and palladium(II) complexes (PtO, PdO) and mononuclear thiazolidine derivative complexes (PtT, PdT) was described. Characterization was performed by elemental analysis, infrared, UV-visible, 1H, 13C, 195Pt NMR spectra, MS spectroscopy and single crystal X-ray diffraction. The cytotoxicity by MTT assay against tumor and normal cell lines with or without extracellular GSH was also investigated. In general, mononuclear complexes containing thiazolidine-adamantane ligands were more cytotoxic than oxadiazole-adamantane derivatives. PtT complex proved to be as active as cisplatin. Dinuclear compounds were considered inactive to cells in evaluated conditions, due to their high stability with ligands in a chelated and bridged way. Results suggest that GSH cannot be considered a target. DNA- and BSA-binding interactions were evaluated using UV-visible and fluorescence spectroscopy, intercalating dyes and molecular docking. Upon coordination to platinum(II), the cytotoxic effect was appreciably improved against tested cell lines, in comparison to free thiazolidine ligand. Comparing thiazolidine derivatives, it is noticeable that the less active compound (PdT) presents stronger interaction with BSA, while PtT has the weaker interaction with BSA and relatively strong binding to isolated DNA, resulting in the most cytotoxic complex. This work shows that the presence of metal is significant but it should be available for interaction. The high lability of palladium complex made this stay retainable in BSA and two metal atoms do not increase activity if it is not able to do any interaction.

中文翻译：

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含有金刚烷-唑配体的单核和双核铂和钯配合物：DNA和BSA相互作用和细胞毒性。

描述了二核恶二唑-金刚烷铂（II）和钯（II）配合物（PtO，PdO）和单核噻唑烷衍生物配合物（PtT，PdT）的合成。通过元素分析，红外，紫外可见，1H，13C，195Pt NMR光谱，MS光谱和单晶X射线衍射进行表征。还研究了MTT法对有或没有细胞外GSH的肿瘤和正常细胞系的细胞毒性。通常，含有噻唑烷-金刚烷配体的单核复合物比恶二唑-金刚烷衍生物具有更高的细胞毒性。事实证明，PtT复合物的活性与顺铂相同。在评估的条件下，双核化合物被认为对细胞无活性，因为它们以螯合和桥接的方式对配体具有很高的稳定性。结果表明，谷胱甘肽不能被视为目标。DNA和BSA的结合相互作用使用紫外可见光谱和荧光光谱，嵌入染料和分子对接进行评估。与游离的噻唑烷配体相比，与铂（II）配位后，对受试细胞系的细胞毒性作用明显改善。比较噻唑烷衍生物，值得注意的是，活性较低的化合物（PdT）与BSA的相互作用更强，而PtT与BSA的相互作用较弱，并且与分离的DNA的结合相对较强，导致了最具细胞毒性的复合物。这项工作表明，金属的存在很重要，但应该可以相互作用。钯络合物的高不稳定性使它可以在BSA中保留，如果两个金属原子不能发生任何相互作用，则不会增加活性。