配体和核数对环金属化 C^N^C 铂(II)配合物细胞毒性的影响。
Influence of Ligand and Nuclearity on the Cytotoxicity of Cyclometallated C^N^C Platinum(II) Complexes.
机构信息
School of Chemistry and Biosciences, Faculty of Life Sciences, University of Bradford, Bradford, West Yorkshire, BD7 1DP, UK.
School of Chemistry, University of East Anglia, Norwich Research Park, Norwich, NR4 7TJ, UK.
出版信息
Chemistry. 2020 Nov 20;26(65):14938-14946. doi: 10.1002/chem.202002517. Epub 2020 Oct 15.
A series of cyclometallated mono- and di-nuclear platinum(II) complexes and the parent organic ligand, 2,6-diphenylpyridine 1 (HC^N^CH), have been synthesized and characterized. This library of compounds includes [(C^N^C)Pt (L)] (L=dimethylsulfoxide (DMSO) 2 and triphenylphosphine (PPh ) 3) and [((C^N^C)Pt ) (L')] (where L'=N-heterocycles (pyrazine (pyr) 4, 4,4'-bipyridine (4,4'-bipy) 5 or diphosphine (1,4-bis(diphenylphosphino)butane (dppb) 6). Their cytotoxicity was assessed against four cancerous cell lines and one normal cell line, with results highlighting significantly increased antiproliferative activity for the dinuclear complexes (4-6), when compared to the mononucleated species (2 and 3). Complex 6 is the most promising candidate, displaying very high selectivity towards cancerous cells, with selectivity index (SI) values >29.5 (A2780) and >11.2 (A2780cisR), and outperforming cisplatin by >4-fold and >18-fold, respectively.
已合成并表征了一系列偕二膦配体单核和双核铂(II)配合物及母体有机配体 2,6-二苯基吡啶 1（HC^N^CH）。该化合物库包括[(C^N^C)Pt (L)]（L=二甲亚砜（DMSO）2 和三苯基膦（PPh 3））和[((C^N^C)Pt ) (L')]（其中 L'=杂环（吡嗪（pyr）4、4,4'-联吡啶（4,4'-bipy）5 或双膦（1,4-双（二苯基膦基）丁烷（dppb）6）。对四种癌细胞系和一种正常细胞系进行了它们的细胞毒性评估，结果表明双核配合物（4-6）与单核配合物（2 和 3）相比，具有明显提高的抗增殖活性。配合物 6 是最有前途的候选物，对癌细胞具有非常高的选择性，选择性指数（SI）值>29.5（A2780）和>11.2（A2780cisR），分别比顺铂高>4 倍和>18 倍。
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