摘要
背景:顺铂的发现及其后续研究揭示了含二氮基的部分对金属配合物抗癌作用的重要性。此外,某些二胺配体单独表现出细胞毒性,有助于相应复合物的整体活性。 目的:综述金属配合物与不同类型二胺配体的抗癌作用、选择性及作用机制的最新研究进展。 方法:通过与有机配体和/或传统铂基化疗药物的比较,分析脂肪族无环、脂肪族环和芳香二胺配体对不同金属离子金属配合物的抗癌活性和选择性/毒性的贡献。 结果:脂肪族无环二胺配体主要存在于铂配合物中。脂肪族环二胺是Pt(II)、Ru(II)和Au(III)配合物的一部分,而芳香二胺配体则存在于Pt(II)、Ru(II)、Pd(II)和Ir(III)配合物中。金属离子的类型和氧化态对脂族无环二胺配合物的细胞毒性有很大影响。有机配体的亲脂性取决于烷基侧链的长度和结构,决定了它们的细胞摄取,其中edda和eddp/eddip配体在这方面最有用。脂肪族环二胺配体提高了草酸铂类配合物的活性/毒性比。芳香族二胺配体的配合物的抗癌机制仍未被探索。所研究的复合物主要导致细胞凋亡或坏死死亡。 结论:含二胺配体的金属配合物是替代传统铂类化疗药物的有效、选择性强的选择。还需要进一步的研究来揭示它们的化学物理性质和生物活性背后的分子机制。
关键词: 金属络合物,二胺配体,抗肿瘤,离体,毒性。
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