Novel binuclear copper(II) complexes with sulfanylpyrazole ligands: synthesis, crystal structure, fungicidal, cytostatic, and cytotoxic activity.

IF 2.9 3区 生物学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY Metallomics Pub Date : 2024-06-04 DOI:10.1093/mtomcs/mfae024
Vnira R Akhmetova, Nail S Akhmadiev, Aidar T Gubaidullin, Aida I Samigullina, Andrey B Glazyrin, Rais A Sadykov, Diana V Ishmetova, Yulia V Vakhitova
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Abstract

New binuclear copper(II) [Cu(II)] tetraligand complexes (six examples) with sulfanylpyrazole ligands were synthesized. Electron spin resonance (ESR) studies have shown that in solution the complexes are transformed to the mononuclear one. Fungicidal properties against Candida albicans were found for the Cu complexes with benzyl and phenyl substituents. An in vitro evaluation of the cytotoxic properties of Cu chelates against HEK293, Jurkat, MCF-7, and THP-1 cells identified the Cu complex with the cyclohexylsulfanyl substituent in the pyrazole core as the lead compound, whereas the Cu complex without a sulfur atom in the pyrazole ligand had virtually no cytotoxic or fungicidal activity. The lead Cu(II) complex was more active than cisplatin. Effect of the S-containing Cu complex on apoptosis and cell cycle distribution has been investigated as well.

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具有硫酰吡唑配体的新型双核铜(II)配合物:合成、晶体结构、杀菌、细胞抑制和细胞毒性活性。
我们合成了带有硫酰吡唑配体的新双核铜(II)四配体络合物(六个实例)。EPR 研究表明,这些配合物在溶液中会转变为单核配合物。研究发现,具有苄基和苯基取代基的铜配合物对白色念珠菌有杀菌作用。通过体外评估铜螯合物对 Hek293、Jurkat、MCF-7 和 THP-1 细胞的细胞毒性特性,发现吡唑核心中含有环己基硫代物的铜络合物是主要化合物,而吡唑配体中没有硫原子的铜络合物几乎没有细胞毒性或杀真菌活性。铅 Cu(II) 复合物的活性高于顺铂。此外,还研究了含 S 的铜络合物对细胞凋亡和细胞周期分布的影响。
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来源期刊
Metallomics
Metallomics 生物-生化与分子生物学
CiteScore
7.00
自引率
5.90%
发文量
87
审稿时长
1 months
期刊介绍: Global approaches to metals in the biosciences
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