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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Influence of carboxylic acid functionalities in ruthenium (II) polypyridyl complexes on DNA binding, cytotoxicity and antioxidant activity: Synthesis, structure and in vitro anticancer activity
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Influence of carboxylic acid functionalities in ruthenium (II) polypyridyl complexes on DNA binding, cytotoxicity and antioxidant activity: Synthesis, structure and in vitro anticancer activity

机译:钌(II)聚吡啶基配合物中羧酸官能团对DNA结合,细胞毒性和抗氧化活性的影响:合成,结构和体外抗癌活性

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摘要

Four new Ru(II) complexes [RuHCl(bpy)(PPh3)(CO)] (1), [RuHCl(bpy)(AsPh3)(CO)] (2) (bpy = 2,2′-bipyridine), [RuCl(HL)(PPh3)2(CO)] (3) and [RuCl(HL)(AsPh 3)2(CO)] (4) (HL = 2,2′-bipyridine-4,4′- dicarboxylic acid) were synthesized and characterized. X-ray diffraction was used to characterize 3 in solid state. The interactions of these complexes with DNA were explored by different techniques which revealed that the complexes could bind to CT-DNA through non-intercalation. The in vitro cytotoxic and antioxidant activities of the complexes validated against a panel of cancer cell lines and free radicals showed that 3 and 4 possess quite high anticancer and antioxidant activities over 1, 2 and standard drugs. An apparent dependence of biological activities on incorporation of COOH in bipyridine moiety was noticed: Inclusion of COOH caused significant differences in DNA binding, cytotoxicity and antioxidant activity.
机译:四个新的Ru(II)络合物[RuHCl(bpy)(PPh3)(CO)](1),[RuHCl(bpy)(AsPh3)(CO)](2)(bpy = 2,2'-联吡啶),[ RuCl(HL)(PPh3)2(CO)](3)和[RuCl(HL)(AsPh 3)2(CO)](4)(HL = 2,2'-联吡啶-4,4'-二羧酸)进行合成和表征。 X射线衍射用于表征固态的3。通过不同的技术探索了这些复合物与DNA的相互作用,揭示了这些复合物可以通过非嵌入方式与CT-DNA结合。针对一组癌细胞系和自由基进行了验证的复合物的体外细胞毒性和抗氧化活性表明,与1、2和标准药物相比,3和4具有相当高的抗癌和抗氧化活性。注意到生物活性对联吡啶部分中COOH掺入的明显依赖性:包含COOH引起DNA结合,细胞毒性和抗氧化活性方面的显着差异。

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