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Biological Investigations of Ru(II) Complexes with Diverse β-Diketone Ligands
European Journal of Inorganic Chemistry ( IF 2.2 ) Pub Date : 2021-07-21 , DOI: 10.1002/ejic.202100468 Raphael T Ryan 1 , Dmytro Havrylyuk 1 , Kimberly C Stevens 1 , L Henry Moore 2 , Sean Parkin 1 , Jessica S Blackburn 2 , David K Heidary 1 , John P Selegue 1 , Edith C Glazer 1
European Journal of Inorganic Chemistry ( IF 2.2 ) Pub Date : 2021-07-21 , DOI: 10.1002/ejic.202100468 Raphael T Ryan 1 , Dmytro Havrylyuk 1 , Kimberly C Stevens 1 , L Henry Moore 2 , Sean Parkin 1 , Jessica S Blackburn 2 , David K Heidary 1 , John P Selegue 1 , Edith C Glazer 1
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The β-diketone scaffold is a commonly used synthetic intermediate, and is a functional group found in natural products such as curcuminoids. This core structure can also act as a chelating ligand for a variety of metals. In order to assess the potential of this scaffold for medicinal inorganic chemistry, seven different κ2-O,O’-chelating ligands were used to construct Ru(II) complexes with polypyridyl co-ligands, and their biological activity was evaluated. The complexes demonstrated promising structure-dependent cytotoxicity. Three complexes maintained high activity in a tumor spheroid model, and all complexes demonstrated low in vivo toxicity in a zebrafish model. From this series, the best compound exhibited a ∼30-fold window between cytotoxicity in a 3-D tumor spheroid model and potential in vivo toxicity. These results suggest that κ2-O,O’-ligands can be incorporated into Ru(II)-polypyridyl complexes to create favorable candidates for future drug development.
中文翻译：
Ru(II) 与多种 β-二酮配体配合物的生物学研究
β-二酮支架是一种常用的合成中间体，是姜黄素等天然产物中发现的官能团。该核心结构还可以充当多种金属的螯合配体。为了评估该支架在药物无机化学中的潜力，使用七种不同的κ 2 -O,O'-螯合配体与聚吡啶基辅助配体构建Ru(II)配合物，并评估其生物活性。该复合物表现出有希望的结构依赖性细胞毒性。三种复合物在肿瘤球体模型中保持高活性，并且所有复合物在斑马鱼模型中表现出低体内毒性。从该系列中，最好的化合物在 3-D 肿瘤球体模型中的细胞毒性与潜在的体内毒性之间表现出约 30 倍的窗口。这些结果表明κ 2 -O,O'-配体可以掺入Ru(II)-聚吡啶复合物中，为未来的药物开发创造有利的候选物。
更新日期：2021-09-15
中文翻译：
Ru(II) 与多种 β-二酮配体配合物的生物学研究
β-二酮支架是一种常用的合成中间体，是姜黄素等天然产物中发现的官能团。该核心结构还可以充当多种金属的螯合配体。为了评估该支架在药物无机化学中的潜力，使用七种不同的κ 2 -O,O'-螯合配体与聚吡啶基辅助配体构建Ru(II)配合物，并评估其生物活性。该复合物表现出有希望的结构依赖性细胞毒性。三种复合物在肿瘤球体模型中保持高活性，并且所有复合物在斑马鱼模型中表现出低体内毒性。从该系列中，最好的化合物在 3-D 肿瘤球体模型中的细胞毒性与潜在的体内毒性之间表现出约 30 倍的窗口。这些结果表明κ 2 -O,O'-配体可以掺入Ru(II)-聚吡啶复合物中，为未来的药物开发创造有利的候选物。
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