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首页> 外文期刊>Journal of biological inorganic chemistry: JBIC: a publication of the Society of Biological Inorganic Chemistry >Metals in medicine: metal-related diseases-Oxicams as bioactive ligand systems in anticancer Ru~(II)(p-cymene) complexes
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Metals in medicine: metal-related diseases-Oxicams as bioactive ligand systems in anticancer Ru~(II)(p-cymene) complexes

机译：药物中的金属：与金属有关的疾病-Oxicams作为抗癌Ru〜（II）（p-cymene）配合物中的生物活性配体系统

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摘要

Bioorganometallic chemistry provides an excellent platform to incorporate drug-like properties in molecules. In recent years, metal arene complexes have been extensively studies for the design of metallodrugs. The most successful examples are RAPTA-C and RM175 [1]. Despite small difference in their structures, both exhibited contrasting biological activity and modes of action. RM175 displayed in vitro anticancer activity similar to that of cisplatin; while RAPTA-C inhibits metastasis in vivo. As evident from X-ray crystallographic experiments, RM175 prefers to bind to DNA while RAPTA-C has high affinity to histone proteins of the nucleosome core particle [2]. This demonstrates that a small structural variation can dramatically alter the reactivity of compounds with cellular targets and hence alter their biological activity. Coordination of a biologically active ligand to a metal center may result in enhanced activity due to synergetic effects. The use of ligands with anti-inflammatory properties may improve the bioactivity of the Ru arene scaffold. As oxicams are known for their anti-inflammatory properties, herein we report the synthesis and characterization of Ru~(II)(p-cymene) complexes of oxicamderived ligands. Their hydrolytic stability, reactivity with biomolecules and in vitro antiproliferative activity will be discussed.
机译：生物有机金属化学提供了一个极好的平台，可将类似药物的特性整合到分子中。近年来，金属芳烃配合物已被广泛用于金属药物的设计。最成功的例子是RAPTA-C和RM175 [1]。尽管它们的结构差异很小，但两者均显示出相反的生物活性和作用方式。 RM175的体外抗癌活性与顺铂相似。而RAPTA-C可抑制体内转移。从X射线晶体学实验可以明显看出，RM175倾向于与DNA结合，而RAPTA-C对核小体核心颗粒的组蛋白具有高亲和力[2]。这表明小的结构变化可以显着改变化合物与细胞靶标的反应性，从而改变其生物学活性。由于协同作用，生物活性配体与金属中心的配位可导致活性增强。具有抗炎特性的配体的使用可以改善钌芳烃支架的生物活性。由于奥昔康素以其抗炎特性而闻名，因此我们在此报道了奥昔康衍生的配体的Ru〜（II）（对伞花烃）复合物的合成和表征。将讨论它们的水解稳定性，与生物分子的反应性和体外抗增殖活性。

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