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杂环卡宾铂(IV)作为金属药物候选物:合成及 Pt NMR 化学位移趋势。

-Heterocyclic Carbene Platinum(IV) as Metallodrug Candidates: Synthesis and Pt NMR Chemical Shift Trend.

机构信息

Institut de Physique et Chimie des Matériaux de Strasbourg, Université de Strasbourg-CNRS UMR7504, 23 rue du Loess, BP 43 CEDEX 2, 67034 Strasbourg, France.

Service de RMN, Fédération de Chimie Le Bel, Université de Strasbourg, CNRS FR2010, 1 rue Blaise Pascal, BP 296R8, CEDEX, 67008 Strasbourg, France.

出版信息

Molecules. 2020 Jul 9;25(14):3148. doi: 10.3390/molecules25143148.

Abstract

A series of octahedral platinum(IV) complexes functionalized with both -heterocyclic carbene (NHC) ligands were synthesized according to a straightforward procedure and characterized. The coordination sphere around the metal was varied, investigating the influence of the substituted NHC and the amine ligand in trans position to the NHC. The influence of those structural variations on the chemical shift of the platinum center were evaluated by Pt NMR. This spectroscopy provided more insights on the impact of the structural changes on the electronic density at the platinum center. Investigation of the in vitro cytotoxicities of representative complexes were carried on three cancer cell lines and showed IC values down to the low micromolar range that compare favorably with the benchmark cisplatin or their platinum(II) counterparts bearing NHC ligands.

摘要

一系列具有杂环卡宾 (NHC) 配体的八面体铂 (IV) 配合物是根据简单的程序合成并进行了表征。金属周围的配位球发生了变化,研究了取代的 NHC 和 NHC 反位的胺配体的影响。通过 Pt NMR 评估了这些结构变化对铂中心化学位移的影响。该光谱提供了更多关于结构变化对铂中心电子密度影响的见解。对代表性配合物的体外细胞毒性进行了研究,结果表明,在三种癌细胞系中,IC 值低至低微摩尔范围,与顺铂或具有 NHC 配体的铂 (II) 同类物的基准值相比具有优势。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d874/7397185/dd8334600402/molecules-25-03148-sch001.jpg

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