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首页> 外文期刊>Cogent Chemistry >Antiproliferative, DNA cleavage, and ADMET study of substituted 2-(1-benzofuran-2-yl) quinoline-4-carboxylic acid and its esters
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Antiproliferative, DNA cleavage, and ADMET study of substituted 2-(1-benzofuran-2-yl) quinoline-4-carboxylic acid and its esters

机译：取代的2-（1-苯并呋喃-2-基）喹啉-4-羧酸及其酯的抗增殖，DNA切割和ADMET研究

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Synthesis, anti-proliferative, DNA cleavage, and in silico ADMET studies of 2-(1-benzofuran-2-yl) quinoline-4-carboxylic acids and their resultant esters in acid catalyzed medium have been investigated. The synthesized compounds are characterized by UV, IR, ~(1)H NMR, ~(13)C NMR, and mass spectral analysis. The electrophoretic DNA cleavage studies on λ-DNA (Eco-RI/Hinda-III double digest) using agarose gel method and the antiproliferative activity was carried out by MTT assay on five different human cancer cell lines (Chronic Myelogenous Leukemia (K562), Breast Cancer (MCF-7), Cervical Cancer (HeLa), Colorectal Adino carcinoma (Colo 205), and Hepato cellular carcinoma (HepG2)). Doxorubicin is taken as standard for comparison. The cleavage study indicated that molecules (3b–6a and 7b–8c) did cleave the DNA completely with no trace of fragments. The molecules (6b, 6c and 7a) have appeared to cleave DNA partially and assessed by comparing the bands appeared in control and test compounds at 100?μg concentration. The MTT antiproliferative activity of the synthesized derivatives at a concentration of 10?mM screened that out of the five cancer cell lines tested, the compounds 8b (25.97%, MCF-7), 7a (25.36%, Colo 205), and 7b (24.22%, HePG) showed considerable degree of activity at a very low concentration. The molecules were active against MCF-7, Colo 205, and HepG. The molecules exhibited acceptable range in in silico ADMET prediction, significant DNA cleavage, and antiproliferative properties. The study further provides identification of possible lead moiety as an antiproliferative agent.
机译：已经研究了在酸催化介质中2-（1-苯并呋喃-2-基）喹啉-4-羧酸及其合成的酯的合成，抗增殖，DNA切割和计算机模拟ADMET研究。合成的化合物通过UV，IR，〜（1）H NMR，〜（13）C NMR和质谱分析进行表征。使用琼脂糖凝胶法对λ-DNA（Eco-RI / Hinda-III双酶切）进行电泳DNA切割研究，并通过MTT分析对五种不同的人类癌细胞系（慢性粒细胞白血病（K562），乳腺癌）进行了抗增殖活性癌症（MCF-7），宫颈癌（HeLa），结直肠阿迪诺癌（Colo 205）和肝细胞癌（HepG2））。以阿霉素为标准进行比较。切割研究表明，分子（3b-6a和7b-8c）确实完全切割了DNA，没有任何片段。分子（6b，6c和7a）似乎能部分切割DNA，并通过比较浓度为100？μg的对照化合物和测试化合物中的条带来评估。合成衍生物在10？mM的浓度下的MTT抗增殖活性筛选出了所测试的5种癌细胞系中的化合物8b（25.97％，MCF-7），7a（25.36％，Colo 205）和7b（ 24.22％（HePG）​​在非常低的浓度下显示出相当程度的活性。这些分子对MCF-7，Colo 205和HepG具有活性。这些分子在计算机模拟ADMET预测中显示出可接受的范围，显着的DNA裂解和抗增殖特性。该研究进一步提供了可能的铅部分作为抗增殖剂的鉴定。

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