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含吡啶酮-咪唑配体的抗增殖水溶性单核和双核钌配合物

Antiproliferative Water-Soluble Mono- and Binuclear Ruthenium Complexes with Pyridone-Imidazole Ligands.

作者信息

Shutkov Ilya A, Melnichuk Nikolai A, Ovakimyan Sofya A, Mazur Dmitrii M, Borisova Nataliya E, Kuznetsov Maxim L, Godovikov Ivan A, Lyssenko Konstantin A, Yakovlev Dmitrii S, Spasov Alexander A, Milaeva Elena R, Nazarov Alexey A

机构信息

Department of Chemistry, M.V. Lomonosov Moscow State University, Leninskie Gory 1/3, 119991 Moscow, Russia.

Centro de Química Estrutural, Institute of Molecular Sciences, Departamento de Engenharia Química, Instituto Superior Técnico, Universidade de Lisboa, 1049-001 Lisboa, Portugal.

出版信息

Int J Mol Sci. 2025 May 29;26(11):5214. doi: 10.3390/ijms26115214.

Abstract

In this study, we synthesized and characterized new imidazole ligands containing pyridone groups, as well as mononuclear and binuclear ruthenium complexes, which are a new class of water-soluble metallacycles. We studied the antiproliferative activity of these compounds in vitro using the MTT assay on a panel of human cancer cell lines and on primary rat fibroblasts, where we observed a complete absence of cytotoxicity up to a concentration of 1000 µM. For the binuclear metallocycle compounds, we investigated their solubility in water, resistance to hydrolysis, and ability to induce apoptosis in tumor cells.

摘要

在本研究中,我们合成并表征了含吡啶酮基团的新型咪唑配体以及单核和双核钌配合物,它们是一类新型的水溶性金属环。我们使用MTT法在一组人类癌细胞系和原代大鼠成纤维细胞上体外研究了这些化合物的抗增殖活性,在高达1000 µM的浓度下未观察到细胞毒性。对于双核金属环化合物,我们研究了它们在水中的溶解度、抗水解性以及诱导肿瘤细胞凋亡的能力。

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