首页> 外文期刊>RSC Advances >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
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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:具有有效的抗增殖活性和增强的LDH和NO释放的3-乙酰基-7-甲氧基香豆素Schiff碱及其Ru(II)金属盐的研究

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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了3-乙酰基-7-甲氧基香豆素-4 N 取代的硫代半脲的新型环金属钌( II )配合物。配体H 2 L 1-3 和配合物(1、2和4)的晶体结构为由X射线晶体学证实。分析表明,配体在吡喃环的C(4)碳原子处经历了C–H活化,并通过C,N和S原子的结合以三齿形式起作用。进行了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。在插层结合模式下观察到与DNA的良好结合亲和力,这通过EB置换和粘度测量研究得到了进一步证实。发现使用BSA / HSA的淬灭机理是静态的。进行了三维(3D)荧光测量,以验证血清白蛋白中的微环境变化。他们的抗氧化倾向和抗微生物研究坚持认为这些化合物显示出良好的活性谱。评估它们对MCF-7(人类乳腺癌)和A549(人类肺癌)细胞系的抗癌潜能表明,该复合物的活性优于配体和顺铂。此外,LDH和NO释放测定的结果支持了化合物的细胞毒性性质。通过针对非癌细胞系HaCaT(人类正常角质形成细胞)进行测试,可以确定化合物的无毒性质。

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