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新型铂(II)三唑硫代半卡巴腙配合物:其反应活性及潜在抗肿瘤作用分析

New Platinum(II) Triazole Thiosemicarbazone Complexes: Analysis of Their Reactivity and Potential Antitumoral Action.

作者信息

Matesanz Ana I, Herrero Jorge M, Faraco Eva J, Cubo Leticia, Quiroga Adoracion G

机构信息

Inorganic Chemistry Department, Universidad Autónoma de Madrid, Ciudad Universitaria de Cantoblanco, 28049, Madrid, Spain.

Institute for Advanced Research in Chemical Sciences (IAdChem), Universidad Autónoma de Madrid, Ciudad Universitaria de Cantoblanco, 28049, Madrid, Spain.

出版信息

Chembiochem. 2020 Apr 17;21(8):1226-1232. doi: 10.1002/cbic.201900545. Epub 2020 Jan 23.

Abstract

The synthesis and characterization of three new platinum complexes, with 3,5-diacetyl-1,2,4-triazole bis(4-N-isopropylthiosemicarbazone) as a ligand, are reported. The specific conditions under which solvent coordination takes place are reported and the X-ray structure of the complex with one solvent molecule of dimethyl sulfoxide is resolved. Analysis of the reactivity of these platinum compounds aids in finding the best solution profile for biological investigations. Then, the interactions of the complexes with biological models, such as calf-thymus DNA, are studied by using UV spectroscopy and tracking the changes in electrophoretic mobility produced in the supercoiled plasmid DNA model. Initial screening of these potential antitumoral compounds indicates possible selective antitumoral action.

摘要

报道了三种以3,5-二乙酰基-1,2,4-三唑双(4-N-异丙基硫代氨基脲)为配体的新型铂配合物的合成与表征。报道了发生溶剂配位的具体条件,并解析了含有一个二甲基亚砜溶剂分子的配合物的X射线结构。对这些铂化合物反应活性的分析有助于找到生物研究的最佳溶液条件。然后,通过紫外光谱法并跟踪超螺旋质粒DNA模型中产生的电泳迁移率变化,研究了这些配合物与生物模型(如小牛胸腺DNA)的相互作用。对这些潜在抗肿瘤化合物的初步筛选表明可能具有选择性抗肿瘤作用。

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