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首页> 美国卫生研究院文献>other >Design Synthesis and Characterisation of New Chimeric Ruthenium(II)-Gold(I) Complexes as Improved Cytotoxic Agents
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Design Synthesis and Characterisation of New Chimeric Ruthenium(II)-Gold(I) Complexes as Improved Cytotoxic Agents

机译：新的嵌合钌（II）-金（I）配合物作为改进的细胞毒剂的设计合成和表征

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摘要

Two heterobimetallic complexes, i.e. [RuCl2(p-cymene)(µ-dppm)AuC] (>1) and [RuCl2(p-cymene)(µ-dppm)Au S(thiazoline)] (>3), based on known cytotoxic [Ru(p-cymene)Cl2(PR3)] and [AuX(PR3)] (X = Cl, SR) molecular scaffolds, with the diphosphane linker 1,1-bis(diphenylphosphino) methane, dppm, were conveniently prepared and characterised. Remarkably, the new compounds manifested a more favourable in vitro pharmacological profile toward cancer cells than individual ruthenium and gold species being either more cytotoxic or more selective. The interactions of the study compounds with (pBR322) DNA and their inhibitory effects on cathepsin B were also assessed. In addition, their reactivity toward suitable models of protein targets was explored and clear evidence gained for disruption of the bimetallic motif and for protein binding of monometallic fragments. Overall, the data reported here strongly support the concept of multifunctional heterometallic compounds as “improved” candidate agents for cancer treatment. The mechanistic and pharmacological implications of the present findings are discussed.
机译：两种杂双金属配合物，即[RuCl2（p-cymene）（µ-dppm）AuC]（> 1 ）和[RuCl2（p-cymene）（µ-dppm）Au S（噻唑啉）]（< strong> 3 ），基于已知的细胞毒性[Ru（p-cymene）Cl2（PR3）]和[AuX（PR3）]（X = Cl，SR）分子支架，并带有二膦连接基1,1-可方便地制备和表征双（二苯基膦基）甲烷dppm。值得注意的是，新化合物对癌细胞的体外药理作用要比单个钌和金物质更具细胞毒性或更具选择性。还评估了研究化合物与（pBR322）DNA的相互作用及其对组织蛋白酶B的抑制作用。此外，探索了它们对合适的蛋白质靶模型的反应性，并获得了破坏双金属基序和结合单金属片段的明确证据。总体而言，此处报告的数据强烈支持多功能异金属化合物作为癌症治疗“改良”候选药物的概念。讨论了本研究结果的机制和药理意义。

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