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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Ruthenium arene complexes bearing naphthyl-substituted 1,3-dioxoindan-2-carboxamides ligands for G-quadruplex DNA recognition
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Ruthenium arene complexes bearing naphthyl-substituted 1,3-dioxoindan-2-carboxamides ligands for G-quadruplex DNA recognition

机译：钌芳烃配合物轴承萘基取代的1,3-二氧茚满-2-甲酰胺配体，用于G-Quadrepled DNA识别

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Quadruplex nucleic acids-DNA/RNA secondary structures formed in guanine rich sequences-proved to have key roles in the biology of cancers and, as such, in recent years they emerged as promising targets for small molecules. Many reports demonstrated that metal complexes can effectively stabilize quadruplex structures, promoting telomerase inhibition, downregulation of the expression of cancer-related genes and ultimately cancer cell death. Although extensively explored as anticancer agents, studies on the ability of ruthenium arene complexes to interact with quadruplex nucleic acids are surprisingly almost unknown. Herein, we report on the synthesis and characterization of four novel Ru(II) arene complexes with 1,3-dioxoindan-2-carboxamides ligands bearing pendant naphthylgroups designed to bind quadruplexes by both stacking and coordinating interactions. We show how improvements on the hydrolytic stability of such complexes, by substituting the chlorido leaving ligand with pyridine, have a dramatic impact on their interaction with quadruplexes and on their cytotoxicity against ovarian cancer cells.
机译：在富含富含血红素序列中形成的Quadreplex核酸-DNA / RNA二次结构 - 证明在癌症的生物学中具有关键作用，并且因此，近年来它们作为对小分子的有前途的靶标。许多报道表明，金属配合物可以有效地稳定四边形结构，促进端粒酶抑制，下调癌症相关基因的表达，最终癌细胞死亡。虽然广泛探索为抗癌剂，但研究钌芳烃配合物与四核酸相互作用的能力令人惊讶地几乎未知。在此，我们报告了四种新型ru（II）芳烃配合物的合成和表征用1,3-二氧茚-2-甲酰胺配体轴承萘甲基族配体，其轴承萘曲基设计成通过堆叠和协调相互作用结合四边形。我们展示了如何改善这种复合物的水解稳定性，通过将氯通与吡啶替换为吡啶，对其与卵巢癌细胞的相互作用具有显着的影响，对卵巢癌细胞进行细胞毒性。

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