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Exploring diversity in platinum(iv) N-heterocyclic carbene complexes: synthesis, characterization, reactivity and biological evaluation†
Dalton Transactions ( IF 3.5 ) Pub Date : 2018-07-27 00:00:00 , DOI: 10.1039/c8dt02113a Mathilde Bouché 1, 2, 3, 4 , Antoine Bonnefont 4, 5, 6, 7 , Thierry Achard 1, 2, 3, 4 , Stéphane Bellemin-Laponnaz 1, 2, 3, 4
Dalton Transactions ( IF 3.5 ) Pub Date : 2018-07-27 00:00:00 , DOI: 10.1039/c8dt02113a Mathilde Bouché 1, 2, 3, 4 , Antoine Bonnefont 4, 5, 6, 7 , Thierry Achard 1, 2, 3, 4 , Stéphane Bellemin-Laponnaz 1, 2, 3, 4
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Platinum(IV) complexes stabilized by N-heterocyclic carbene ligands of the type [(NHC)PtX4L], where L is a neutral nitrogen-based ligand and X is a halide anion (Br, Cl), were prepared by using straightforward and high-yielding synthetic routes and the scope was extended to amphiphilic derivatives. The complexes were fully characterized and the molecular structure of the three derivatives was determined by single-crystal X-ray analyses. The complexes demonstrated in vitro antiproliferative activities against several cancer cell lines. In particular, a representative Pt(IV) complex, namely, [(NHC)PtCl4(pyridine)], displayed efficient antiproliferative activity against cisplatin-resistant cancer cells. These results were correlated with their physicochemical properties, namely, solubility, stability and redox behavior by means of UV-vis spectroscopy, NMR or cyclic voltammetry, whereas in DMSO/water, these Pt(IV) complexes transform into biologically less active cis[(NHC)PtX2(DMSO)] species, in the presence of a bioreductant such as glutathione which quickly leads to the formation of a biologically active trans[(NHC)PtX2L] complex. Overall, these data show that NHC-Pt(IV) compounds are good candidates as anti-cancer prodrugs.
中文翻译：
探索铂（iv）N-杂环卡宾配合物的多样性：合成，表征，反应性和生物学评估†
通过直接使用[[NHC] PtX 4 L]型的N-杂环卡宾配体稳定的铂（IV）配合物，其中L为中性氮基配体，X为卤化物阴离子（Br，Cl）和高产的合成路线，范围扩大到两亲衍生物。对该配合物进行了充分表征，并通过单晶X射线分析确定了这三种衍生物的分子结构。该复合物显示出对几种癌细胞的体外抗增殖活性。特别地，代表性的Pt（IV）络合物，即[（NHC）PtCl 4（吡啶）]，对顺铂耐药癌细胞显示出有效的抗增殖活性。这些结果与其物理化学性质相关，即通过紫外可见光谱，NMR或循环伏安法测定的溶解度，稳定性和氧化还原行为，而在DMSO /水中，这些Pt（IV）络合物转化为生物活性较低的顺式[[ NHC）PtX 2（DMSO）]物种，在存在生物还原剂（如谷胱甘肽）的情况下，迅速导致形成生物活性的反式[（NHC）PtX 2 L]复合物。总体而言，这些数据表明NHC-Pt（IV）化合物是抗癌前药的良好候选者。
更新日期：2018-07-27
中文翻译：
探索铂（iv）N-杂环卡宾配合物的多样性：合成，表征，反应性和生物学评估†
通过直接使用[[NHC] PtX 4 L]型的N-杂环卡宾配体稳定的铂（IV）配合物，其中L为中性氮基配体，X为卤化物阴离子（Br，Cl）和高产的合成路线，范围扩大到两亲衍生物。对该配合物进行了充分表征，并通过单晶X射线分析确定了这三种衍生物的分子结构。该复合物显示出对几种癌细胞的体外抗增殖活性。特别地，代表性的Pt（IV）络合物，即[（NHC）PtCl 4（吡啶）]，对顺铂耐药癌细胞显示出有效的抗增殖活性。这些结果与其物理化学性质相关，即通过紫外可见光谱，NMR或循环伏安法测定的溶解度，稳定性和氧化还原行为，而在DMSO /水中，这些Pt（IV）络合物转化为生物活性较低的顺式[[ NHC）PtX 2（DMSO）]物种，在存在生物还原剂（如谷胱甘肽）的情况下，迅速导致形成生物活性的反式[（NHC）PtX 2 L]复合物。总体而言，这些数据表明NHC-Pt（IV）化合物是抗癌前药的良好候选者。
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