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Potent Half-Sandwich Iridium(III) and Ruthenium(II) Anticancer Complexes Containing a P^O-Chelated Ligand

机译:有效的半三明治铱(III)和钌(II)抗癌复合物,含有P ^ O螯合配体

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机译:<![CDATA [我们在此报告了一系列铱(III)和钌(II)的合成,表征和抗癌活性[(CP〜(x)/ arene)m(p ^ O)Cl] PF_(6)(M = IR,CP〜(x)=五甲基环戊二烯基(CP *)或其苯基(CP〜(XPH)= C_(5)ME_(4)C_(6)H_(5) (CP〜(Xbiph)= C_(5)Me_(4)C_(6)H_(4)C_(6)H_(5))衍生物; M = Ru,arene = p-cymene( p-cym); P ^ o =膦膦酰胺配体(PPOA))。确定了所有配合物的X射线晶体结构,其中配体可以与金属中心形成六元环。所有复合体都表现出令人瞩目的抗癌活动,朝Hela和A549癌细胞,高于临床抗癌药物顺铂的活动。掺入铱(III)复合物的CP *环上的苯基取代基导致它们的抗癌活动几乎没有变化。这些结果可归因于金属和PPOA配体的组合作用。水解和DNA裂解不是主要的作用机制。这些配合物在NADH的转移氢化至NAD〜(+)中显示出有效的催化活性。另外,复合物[(η〜(5)-C_(5)ME_(5))IR(P ^ O)CL] PF_(6)( 1)和[(η〜(6) - P-CYM)CL] PF_(6)( 4)分别在S和G_(2)/ m相和S期的抑制细胞循环。复合物 1和 4都可以诱导Hela癌细胞的凋亡。还进行了活性氧物质(ROS)和线粒体膜电位测试以探讨作用机制。当复合物的浓度增加时,活性氧物质(ROS)的量显着增加,线粒体膜电位在Hela癌细胞中显着降低。总体而言,细胞应力包括细胞周期扰动,细胞凋亡诱导,ROS水平的增加,并且线粒体膜势的丧失有助于这些配合物的抗癌效力。有趣的是,使用c

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  • 来源
    《Organometallics》 |2018年第17期|共10页
  • 作者单位

    Institute of Anticancer Agents Development and Theranostic Application The Key Laboratory of Life-Organic Analysis and Key Laboratory of Pharmaceutical Intermediates and Analysis of Natural Medicine Department of Chemistry and Chemical Engineering Qufu;

    Institute of Anticancer Agents Development and Theranostic Application The Key Laboratory of Life-Organic Analysis and Key Laboratory of Pharmaceutical Intermediates and Analysis of Natural Medicine Department of Chemistry and Chemical Engineering Qufu;

    Institute of Anticancer Agents Development and Theranostic Application The Key Laboratory of Life-Organic Analysis and Key Laboratory of Pharmaceutical Intermediates and Analysis of Natural Medicine Department of Chemistry and Chemical Engineering Qufu;

    Institute of Anticancer Agents Development and Theranostic Application The Key Laboratory of Life-Organic Analysis and Key Laboratory of Pharmaceutical Intermediates and Analysis of Natural Medicine Department of Chemistry and Chemical Engineering Qufu;

    Institute of Anticancer Agents Development and Theranostic Application The Key Laboratory of Life-Organic Analysis and Key Laboratory of Pharmaceutical Intermediates and Analysis of Natural Medicine Department of Chemistry and Chemical Engineering Qufu;

    Institute of Anticancer Agents Development and Theranostic Application The Key Laboratory of Life-Organic Analysis and Key Laboratory of Pharmaceutical Intermediates and Analysis of Natural Medicine Department of Chemistry and Chemical Engineering Qufu;

    Institute of Anticancer Agents Development and Theranostic Application The Key Laboratory of Life-Organic Analysis and Key Laboratory of Pharmaceutical Intermediates and Analysis of Natural Medicine Department of Chemistry and Chemical Engineering Qufu;

    Institute of Anticancer Agents Development and Theranostic Application The Key Laboratory of Life-Organic Analysis and Key Laboratory of Pharmaceutical Intermediates and Analysis of Natural Medicine Department of Chemistry and Chemical Engineering Qufu;

    Institute of Anticancer Agents Development and Theranostic Application The Key Laboratory of Life-Organic Analysis and Key Laboratory of Pharmaceutical Intermediates and Analysis of Natural Medicine Department of Chemistry and Chemical Engineering Qufu;

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  • 正文语种 eng
  • 中图分类 元素有机化合物;
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