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An investigation on 3-acetyl-7-methoxy-coumarin Schiff bases and their Ru(II) metallates with potent antiproliferative activity and enhanced LDH and NO release

机译:具有效力抗增殖活性的3-乙酰基-7-甲氧基 - 香豆素席克群及其ru(II)金属的研究,增强LDH,没有释放

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摘要

New cyclometallated ruthenium(II) complexes of 3-acetyl-7-methoxycoumarin-4N-substituted thiosemicarbazones were synthesized and characterized by analytical and spectral techniques. The crystal structures of the ligands H2L1-3 and complexes (1, 2 and 4) were confirmed by X-ray crystallography. The analysis showed that the ligands have undergone C-H activation at the C(4) carbon of the pyrone ring and acted in a tridentate fashion by binding through C, N and S atoms. CT-DNA and protein (BSA/HSA) binding studies were carried out to analyze their interaction with biomolecules. Good binding affinity with DNA was observed with intercalative binding mode, which was further confirmed by EB displacement and viscosity measurement studies. The quenching mechanism with BSA/HSA was found to be static. Three dimensional (3D) fluorescence measurements were carried out to validate the micro environmental changes in the serum albumins. Their antioxidant propensity and antimicrobial study insisted that the compounds displayed good spectrum of activity. Evaluation of their anticancer potential against MCF-7 (human breast cancer) and A549 (human lung carcinoma) cell lines revealed that the complexes exhibited better activity than the ligands and cisplatin. Further, the results of LDH and NO release assays supported the cytotoxic nature of the compounds. The non-toxic nature of the compounds was established by testing against the non-cancerous cell line HaCaT (human normal keratinocyte).
机译:通过分析和光谱技术合成新的3-乙酰基-7-甲氧基苏马林-4N取代的硫代硫脲的新的环管炔(II)复合物。通过X射线晶体学证实了配体H 2L1-3和配合物(1,2和4)的晶体结构。该分析表明,配体在吡喃酮环的C(4)碳处经过C-H抗激活,并通过C,N和S原子结合三级时尚作用。进行CT-DNA和蛋白质(BSA / HSA)结合研究以分析它们与生物分子的相互作用。用插入式结合模式观察与DNA的良好结合亲和力,通过EB位移和粘度测量研究进一步证实。发现具有BSA / HSA的猝灭机制是静态的。进行三维(3D)荧光测量以验证血清白化素中的微观环境变化。它们的抗氧化倾向和抗微生物研究坚持认为该化合物显示出良好的活性。评估对MCF-7(人乳腺癌)和A549(人肺癌)细胞系的抗癌潜力揭示了复合物表现出比配体和顺铂的更好的活性。此外,LDH的结果和释放测定的结果支持化合物的细胞毒性。通过针对非癌细胞系HaCAT(人正常角质形成细胞)测试来确定化合物的无毒性质。

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  • 来源
    《RSC Advances》 |2018年第3期|共23页
  • 作者单位

    Bharathiar Univ Dept Chem Coimbatore 641046 Tamil Nadu India;

    Karunya Univ Dept Biosci &

    Technol Coimbatore 641114 Tamil Nadu India;

    Bharathiar Univ Dept Chem Coimbatore 641046 Tamil Nadu India;

    Silsian Univ Dept Crystallog Szkolna 9 PL-40006 Katowice Poland;

    Bharathiar Univ Dept Chem Coimbatore 641046 Tamil Nadu India;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 化学;
  • 关键词

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