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α-三羰基铼(I)与吡啶硫酮配合物的合成、物理化学表征及生物效应评估

Synthesis of a -Tricarbonylrhenium(I) Complex with Pyrithione, Its Physicochemical Characterization, and Assessment of Biological Effects.

作者信息

Rapuš Uroš, Pivarcsik Tamás, Mitrović Ana, Kljun Jakob, Bogdanov Anita, Spengler Gabriella, Meden Anže, Gobec Stanislav, Kos Janko, Enyedy Éva A, Turel Iztok

机构信息

Faculty of Chemistry and Chemical Technology, University of Ljubljana, Večna pot 113, SI-1000 Ljubljana, Slovenia.

Department of Molecular and Analytical Chemistry, Interdisciplinary Excellence Centre, University of Szeged, Dóm tér 7-8., H-6720 Szeged, Hungary.

出版信息

ACS Omega. 2025 Aug 15;10(33):38272-38291. doi: 10.1021/acsomega.5c06647. eCollection 2025 Aug 26.

Abstract

Research on rhenium complexes containing -tricarbonyl fragments has been on the rise in recent decades. Some complexes of this type exhibit advantageous properties that can be utilized in diagnostic and therapeutic applications. Herein, we report on the synthesis, structural characterization, solution speciation, and biological activity with mode of action studies of a new -tricarbonylrhenium-(I) complex with pyrithione ligand -[Re-(CO)(pyrithionato)-(benzonitrile)] (). In an attempt to prepare a stable rhenium-(I) complex with a pyrithionato ligand, several synthesis procedures were investigated and various products were discovered. In solution, the monodentate benzonitrile ligand can be replaced by a coordinating solvent molecule; however, the carbonyl ligands and pyrithione remain bound to the rhenium center. Complex exhibited strong cytotoxic and antibacterial activity and effectively inhibited the growth of the HSV-2 virus. Additionally, complex was also able to inhibit the cathepsin B enzyme (both its endo- and exopeptidase activities). experiments confirmed that complex can interact with cathepsin B near its active site, which may contribute to reduced enzymatic activity.

摘要

近几十年来,对含有 -三羰基片段的铼配合物的研究一直在增加。这类配合物中的一些表现出可用于诊断和治疗应用的有利性质。在此,我们报告一种新的带有吡啶硫酮配体的 -三羰基铼-(I)配合物 -[Re-(CO)(吡啶硫酮基)-(苄腈)] ()的合成、结构表征、溶液形态以及作用方式研究的生物活性。为了制备一种稳定的带有吡啶硫酮基配体的铼-(I)配合物,研究了几种合成方法并发现了各种产物。在溶液中,单齿苄腈配体可被配位溶剂分子取代;然而,羰基配体和吡啶硫酮仍与铼中心结合。配合物 表现出很强的细胞毒性和抗菌活性,并有效抑制了HSV - 2病毒的生长。此外,配合物 还能够抑制组织蛋白酶B(其内切酶和外切酶活性)。 实验证实配合物 可在组织蛋白酶B的活性位点附近与其相互作用,这可能有助于降低酶活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c00e/12391994/ed4e7526495d/ao5c06647_0001.jpg

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