新型 4`官能化双三吡啶钌(II)配合物的合成、表征和生物活性:抗炎活性的进展。

IF 3.6 4区 医学 Q2 CHEMISTRY, MEDICINAL ChemMedChem Pub Date : 2024-10-17 DOI:10.1002/cmdc.202400680
Mohamed Elnagar, Khaled S Abou-El-Sherbini, Safia Samir, Walid Sharmoukh, Mohamed S Abdel-Aziz, Yasser M Shaker
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引用次数: 0

摘要

含有 2,2':6',2''-三联吡啶配体的钌配合物具有多种生物活性,包括 DNA 结合、抗炎、抗菌和抗癌特性,因此已成为很有前途的候选化合物。本研究合成了三种新型 4'-功能化双(特吡啶)钌(II)配合物。这些配合物的一个配体是 4-(2,2':6',2''-三联吡啶-4'-基)苯甲酸,第二个配体是 4'-(2-噻吩基)-2,2':6',2''-三联吡啶、4'-(3,4-二甲氧基苯基)-2,2':6',2''-三联吡啶或 4'-(4-二甲氨基苯基)-2,2':6',2''-三联吡啶。除了通过 1H 和 13C NMR、质谱、吸收和发射光谱进行化学表征外,还测试了这些配合物作为抗炎、抗癌和抗菌剂的生物活性。此外,还利用溶血试验评估了 Ru(II) 复合物的毒性,并将其与双氯芬酸钾和布洛芬进行了比较。生物学评估结果表明,与标准药物相比,这些钌配合物的溶血活性更低,具有良好的治疗潜力。通过抑制白蛋白变性,它们显示出了强大的抗炎作用,同时对癌细胞株具有适度的细胞毒性和广谱抗菌活性。这些发现凸显了 4'-功能化双(特吡啶)钌(II)复合物的多方面生物医学应用,表明它们有潜力进一步发展成为有效、安全的治疗剂。
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Synthesis, Characterization, and Biological Activity of New 4`-Functionalized Bis-Terpyridine Ruthenium(II) Complexes: Anti-inflammatory Activity Advances.

Ruthenium complexes incorporating 2,2':6',2''-terpyridine ligands have emerged as promising candidates due to their versatile biological activities including DNA-binding, anti-inflammatory, antimicrobial, and anticancer properties. In this study, three novel 4'-functionalized bis(terpyridine) ruthenium (II) complexes were synthesized. These complexes feature one ligand as 4-(2,2':6',2''-terpyridine-4'-yl) benzoic acid and the second ligand as either 4'-(2-thienyl)-2,2':6',2''-terpyridine, 4'-(3,4-dimethoxyphenyl)-2,2':6',2''-terpyridine, or 4'-(4-dimethylaminophenyl)-2,2':6',2''-terpyridine. Besides the chemical characterization by 1H and 13C NMR, mass spectrometry, and absorption and emission spectroscopy, the complexes were tested for their biological activity as anti-inflammatory, anticancer, and antimicrobial agents. Moreover, the toxicity of the Ru(II) complexes was assessed and benchmarked against diclofenac potassium and ibuprofen using a haemolysis assay. Biological evaluations demonstrate that these ruthenium complexes exhibit promising therapeutic potential with reduced haemolytic activity compared to standard drugs. They demonstrate substantial anti-inflammatory effects through inhibition of albumin denaturation along with moderate cytotoxicity against cancer cell lines and broad-spectrum antimicrobial activity. These findings highlight the multifaceted biomedical applications of 4'-functionalized bis(terpyridine) ruthenium (II) complexes, suggesting their potential for further development as effective and safe therapeutic agents.

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来源期刊
ChemMedChem
ChemMedChem 医学-药学
CiteScore
6.70
自引率
2.90%
发文量
280
审稿时长
1 months
期刊介绍: Quality research. Outstanding publications. With an impact factor of 3.124 (2019), ChemMedChem is a top journal for research at the interface of chemistry, biology and medicine. It is published on behalf of Chemistry Europe, an association of 16 European chemical societies. ChemMedChem publishes primary as well as critical secondary and tertiary information from authors across and for the world. Its mission is to integrate the wide and flourishing field of medicinal and pharmaceutical sciences, ranging from drug design and discovery to drug development and delivery, from molecular modeling to combinatorial chemistry, from target validation to lead generation and ADMET studies. ChemMedChem typically covers topics on small molecules, therapeutic macromolecules, peptides, peptidomimetics, and aptamers, protein-drug conjugates, nucleic acid therapies, and beginning 2017, nanomedicine, particularly 1) targeted nanodelivery, 2) theranostic nanoparticles, and 3) nanodrugs. Contents ChemMedChem publishes an attractive mixture of: Full Papers and Communications Reviews and Minireviews Patent Reviews Highlights and Concepts Book and Multimedia Reviews.
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