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锌配合物与苯并咪唑衍生物:合成、结构、抗菌活性及潜在抗癌应用。

Zinc Coordination Compounds with Benzimidazole Derivatives: Synthesis, Structure, Antimicrobial Activity and Potential Anticancer Application.

机构信息

Institute of General and Ecological Chemistry, Faculty of Chemistry, Lodz University of Technology, Żeromskiego 116, 90-924 Łódź, Poland.

Department of Pharmaceutical Microbiology, Medical University of Lublin, Chodźki 1, 20-093 Lublin, Poland.

出版信息

Int J Mol Sci. 2022 Jun 13;23(12):6595. doi: 10.3390/ijms23126595.

DOI:10.3390/ijms23126595
PMID:35743039
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9224258/
Abstract

Developing new, smart drugs with the anticancer activity is crucial, especially for cancers, which cause the highest mortality in humans. In this paper we describe a series of coordination compounds with the element of health, zinc, and bioactive ligands, benzimidazole derivatives. By way of synthesis we have obtained four compounds named , , and Analytical analyses (elemental analysis (EA), flame atomic absorption spectrometry (FAAS)), spectroscopic (Fourier transform infrared spectroscopy (FT-IR), mass spectrometry (MS)) and thermogravimetric (TG) methods and the definition of crystal structures were used to explore the nature of bonding and to elucidate the chemical structures. The collected analytical data allowed the determination of the stoichiometry in coordination compounds, thermal stability, crystal structure and way of bonding. The cytotoxicity effect of the new compounds as a potential antitumor agent on the glioblastoma (T98G), neuroblastoma (SK-N-AS) and lung adenocarcinoma (A549) cell lines and human normal skin fibroblasts (CCD-1059Sk) was also determined. Cell viability was determined by the MTT assay. The results obtained confirmed that conversion of ligands into the respective metal complexes significantly improved their anticancer properties. The complexes were screened for antibacterial and antifungal activities. The ADME technique was used to determine the physicochemical and biological properties.

摘要

开发具有抗癌活性的新型智能药物至关重要,特别是对于癌症,癌症是导致人类死亡率最高的疾病。在本文中,我们描述了一系列具有健康元素锌和生物活性配体苯并咪唑衍生物的配位化合物。通过合成,我们获得了四种化合物,分别命名为 、 、 和 。采用分析方法(元素分析(EA)、火焰原子吸收光谱法(FAAS))、光谱法(傅里叶变换红外光谱法(FT-IR)、质谱法(MS))和热重法(TG)以及晶体结构的定义来探索键的性质并阐明化学结构。收集到的分析数据允许确定配位化合物中的化学计量比、热稳定性、晶体结构和键合方式。还测定了新化合物作为潜在抗肿瘤剂对神经母细胞瘤(SK-N-AS)、神经胶质瘤(T98G)和肺腺癌(A549)细胞系和人正常皮肤成纤维细胞(CCD-1059Sk)的细胞毒性作用。通过 MTT 测定法确定细胞活力。结果证实,将配体转化为相应的金属配合物可显著提高其抗癌性能。对这些配合物进行了抗菌和抗真菌活性筛选。ADME 技术用于确定物理化学和生物学性质。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ae6b/9224258/648331b5530c/ijms-23-06595-g005a.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ae6b/9224258/c5aff101e601/ijms-23-06595-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ae6b/9224258/103af2e48798/ijms-23-06595-sch003.jpg
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