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功能化偶氮苯铂(II)配合物作为潜在的抗癌化合物。

Functionalized azobenzene platinum(II) complexes as putative anticancer compounds.

机构信息

Departament de Química, Facultat de Ciències, Universitat Autònoma de Barcelona, 08193-Cerdanyola del Vallès, Barcelona, Spain.

Institut de Biotecnologia i Biomedicina, Departments Bioquímica i Biologia Molecular, Universitat Autònoma de Barcelona, 08193-Cerdanyola del Vallès, Barcelona, Spain.

出版信息

J Biol Inorg Chem. 2021 Jun;26(4):435-453. doi: 10.1007/s00775-021-01865-9. Epub 2021 May 1.

DOI:10.1007/s00775-021-01865-9
PMID:33934217
Abstract

The synthesis and characterization of four platinum(II) complexes using azobenzenes conveniently functionalized as ligands has been carried out. The characteristic photochemical behavior of the complexes due to the presence of azobenzene-type ligands and the role of the ligands in the activation of the complexes has been studied. Their promising cytotoxicity observed in HeLa cells prompted us to study the mechanism of action of these complexes as cytostatic agents. The interaction of the compounds with DNA, studied by circular dichroism, revealed a differential activity of the Pt(II) complexes upon irradiation. The intercalation abilities of the complexes as well as their reactivity with common proteins present in the blood stream allows to confirm some of the compounds obtained as good anticancer candidates.

摘要

已经进行了使用方便地作为配体功能化的偶氮苯合成和表征四种铂(II)配合物。由于存在偶氮苯型配体和配体在配合物的激活中的作用,研究了配合物的特征光化学行为。它们在 HeLa 细胞中观察到的有前途的细胞毒性促使我们研究这些配合物作为细胞抑制剂的作用机制。通过圆二色性研究化合物与 DNA 的相互作用,揭示了辐照下 Pt(II)配合物的不同活性。配合物的插入能力以及它们与血液中常见蛋白质的反应性,证实了一些获得的化合物是良好的抗癌候选物。

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