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首页> 外文期刊>Chemistry: A European journal >Comparison Between Polypyridyl and Cyclometalated Ruthenium(II) Complexes: Anticancer Activities Against 2D and 3D Cancer Models
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Comparison Between Polypyridyl and Cyclometalated Ruthenium(II) Complexes: Anticancer Activities Against 2D and 3D Cancer Models

机译：聚吡啶和环金属化钌（II）配合物之间的比较：对2D和3D癌症模型的抗癌活性。

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摘要

The aim of this study was to illustrate the dramatically different anticancer activities between coordinatively saturated polypyridyl (1a-4a) and cyclometalated (1b-4b) ruthenium(II) complexes. The cyclometalated complexes 1b-4b function as DNA transcription inhibitors, exhibiting switch-on cytotoxicity against a 2D cancer cell monolayer, whereas the polypyridyl complexes 1a-4a are relatively inactive. Moreover, complexes 1b-4b exhibit excellent cytotoxicity against 3D multicellular tumor spheroids (MCTSs), which serve as an intermediate model between in vitro 2D cell monolayers and in vivo 3D solid tumors. The hydrophobicity, efficient cell uptake, and nucleus targeting ability, as well as the high DNA binding affinity of complexes 1b-4b, likely contribute to their enhanced anticancer activity. We surmise that cyclometalation could be a universal approach to significantly enhance the anticancer activity of substituted polypyridyl Ru-II complexes. We also suggest that 3D MCTSs may be a more practical platform for anticancer drug screening than 2D cancer monolayer approaches.
机译：这项研究的目的是说明配位饱和的聚吡啶基（1a-4a）和环金属化（1b-4b）钌（II）配合物之间显着不同的抗癌活性。环金属化的复合物1b-4b充当DNA转录抑制剂，对2D癌细胞单层表现出开启的细胞毒性，而聚吡啶基复合物1a-4a相对没有活性。此外，复合物1b-4b对3D多细胞肿瘤球体（MCTS）表现出优异的细胞毒性，MCTS是体外2D细胞单层与体内3D实体瘤之间的中间模型。疏水性，有效的细胞摄取和细胞核靶向能力以及复合物1b-4b的高DNA结合亲和力可能有助于增强其抗癌活性。我们推测环金属化可能是一种普遍的方法，可以显着增强取代的聚吡啶基Ru-II配合物的抗癌活性。我们还建议，与2D癌症单层方法相比，3D MCTS可能是更实用的抗癌药物筛选平台。

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