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首页> 外文期刊>The Open Medicinal Chemistry Journal >Cytotoxic, DNA Cleavage and Pharmacokinetic Parameter Study of Substituted Novel Furan C-2 Quinoline Coupled 1, 2, 4-Triazole and Its Analogs
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Cytotoxic, DNA Cleavage and Pharmacokinetic Parameter Study of Substituted Novel Furan C-2 Quinoline Coupled 1, 2, 4-Triazole and Its Analogs

机译：新型呋喃C-2喹啉偶联的1,2,4-三唑及其类似物的细胞毒性，DNA切割和药代动力学参数研究

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Background:Furan, quinoline and triazoles are known for their wide spectrum biologically active molecules. A series of novel furan C-2 quinoline and 1, 2, 4-triazole (FQT) coupled hybrids were designed and synthesized to evaluate for their DNA cleavage and cytotoxic studies.Objectives:In this work we describe the synthesis and biological evaluation of furan C-2 quinoline coupled triazoles exposed for cytotoxic and DNA cleavage study.Methods:The electrophoretic DNA cleavage studies on λ-DNA (Eco-RI/Hinda-III double digest) using agarose gelelectrophoresis and the cytotoxic activity were carried out by MTT assay method.Results:The results revealed that, the molecules 7(a-o) did cleave the DNA completely with no trace of fragments at 100 μg concentration, on the other hand, cytotoxic assay was achieved by two different human cancer cell lines (melanoma cell line-A375 and breast cancer cell line MDA-MB 231). Among the synthesized compounds 7a, 7b, 7c and 7k exhibited potent cytotoxic activity with IC50 values ranging from 2.9, 4.0, 7.8 and 5.1 μg/ml against A375 and 6.2, 9.5, 11.3 and 7.3 μg/ml against, MDA-MB 231, respectively.Conclusion:In synthesized compounds 7(a-o) exhibited complete DNA cleavage at 100 μg/ml and the compounds 7a, 7b, 7c and 7k showed very less cytotoxic in nature. The structure activity relationship revealed that, the presence of halogen group/atoms at para position of phenyl ring remarkably enhanced the DNA cleavage and cytotoxic activities among the synthesized compounds.
机译：背景：呋喃，喹啉和三唑以其广谱的生物活性分子而闻名。设计并合成了一系列新型的呋喃C-2喹啉和1，2，4-三唑（FQT）偶联杂合体，以评估其DNA裂解和细胞毒性研究。目的：在这项工作中，我们描述了呋喃的合成和生物学评估方法：采用琼脂糖凝胶电泳法对λ-DNA（Eco-RI / Hinda-III双酶切）进行电泳DNA裂解研究，并采用MTT法测定其细胞毒性，并进行C-2喹啉偶联三唑的细胞毒性和DNA裂解研究。结果：结果表明，在100μg浓度下，分子7（ao）确实完全切割了DNA，没有片段的痕迹，另一方面，通过两种不同的人类癌细胞系（黑色素瘤细胞系- A375和乳腺癌细胞系MDA-MB 231）。在合成的化合物7a，7b，7c和7k中显示出有效的细胞毒性活性，针对A375的IC50值为2.9、4.0、7.8和5.1μg/ ml，针对MDA-MB 231的IC50值为6.2、9.5、11.3和7.3μg/ ml。结论：在合成的化合物7（ao）中，它们以100μg/ ml显示出完全的DNA裂解，并且化合物7a，7b，7c和7k本质上显示出非常小的细胞毒性。结构活性关系表明，在苯环对位的卤素基团/原子的存在显着增强了合成化合物之间的DNA裂解和细胞毒活性。

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