芳基取代(E)- n-苯基-1-(吡啶-3-基)甲亚胺的单核离散Ag(I)配合物:体外生物活性及与生物分子的相互作用

IF 0.8 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY South African Journal of Chemistry-Suid-Afrikaanse Tydskrif Vir Chemie Pub Date : 2023-01-01 DOI:10.17159/0379-4350/2023/v77a08
A. Adeleke, S. Islam, K. Olofinsan, V. Salau, B. Omondi
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引用次数: 1

摘要

在我们对具有潜在药理活性的新型金属药物的持续研究中,合成了三种具有供电子和吸电子官能团的吡啶基亚胺(L1-L3)及其银(I)配合物(1a-3a, 1b-3b和1c-3c)。利用各种分析和光谱分析方法对Ag(I)配合物进行了表征。固体状态下配合物3a和3b的单晶x射线衍射分析证实了它们围绕Ag(I)中心的线性几何结构。用最小抑菌浓度(MIC)法对配合物的体外抗菌性能进行了评价,结果表明,含有Me-或f -取代基的配合物具有更高的活性。铁还原抗氧化能力(FRAP)实验表明,羟基取代配合物具有较高的抗氧化潜力。这些复合物的IC50值为0.86 ~ 2.47 mg mL-1,优于抗坏血酸,IC50值为2.68 mg mL-1。所报道的配合物通过插入模式与CT-DNA结合,对于配体含有OH-取代基的配合物具有显著的结合常数。牛血清白蛋白(BSA)与复合物的结合亲和力从中等到高不等。所研究的甲基取代配合物是很有前途的抗宫颈癌候选物。
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Mononuclear discrete Ag(I) complexes of aryl substituted (E)-N-phenyl-1-(pyridin-3-yl)methanimine: In vitro biological activities and interactions with biomolecules
The synthesis of three pyridinyl imines (L1-L3) with electron-donating and electron-withdrawing functional groups, as well as their silver(I) complexes (1a-3a, 1b-3b and 1c-3c), resulted from our ongoing search for novel metallodrugs with potential pharmacological activity. Various analytical and spectroscopic analyses were used to characterize the Ag(I) complexes. The single crystal X-ray diffraction analysis of complexes 3a and 3b in the solid state confirmed their linear geometry around the Ag(I) center. In vitro antibacterial properties of the complexes evaluated using the minimum inhibitory concentration (MIC) method revealed that complexes containing either a Me- or an F-substituent exhibited greater activity. The ferric-reducing antioxidant power (FRAP) experiment revealed that complexes with hydroxyl substituents have high antioxidant potential. These complexes with IC50 values ranging from 0.86 to 2.47 mg mL-1 outperformed ascorbic acid, with an IC50 of 2.68 mg mL-1. The reported complexes bound to CT-DNA via intercalation mode with significant binding constants for complexes whose ligands bore the OH- substituent. Bovine serum albumin (BSA) binding affinity to the complexes ranges from moderate to high. The studied complexes with methyl substituents are promising anti-cervical cancer candidates.
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来源期刊
CiteScore
3.10
自引率
0.00%
发文量
6
审稿时长
>12 weeks
期刊介绍: Original work in all branches of chemistry is published in the South African Journal of Chemistry. Contributions in English may take the form of papers, short communications, or critical reviews.
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