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首页> 外文期刊>Medicinal chemistry >Synthesis and antiproliferative activity of new coumarin-based benzopyranone derivatives against human tumor cell lines.
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Synthesis and antiproliferative activity of new coumarin-based benzopyranone derivatives against human tumor cell lines.

机译:新的基于香豆素的苯并吡喃酮衍生物的合成及其抗人肿瘤细胞系的活性。

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The synthesis and antiproliferative activity of new coumarin-based benzopyranone derivatives containing basic amino side chain are described. The cytotoxicities against A549 and MCF-7 human cancerous cell lines were determined after 24, 48, 72 h drug exposure employing MTT assay at concentrations ranging from 0-100 muM. The antiproliferative activities of these compounds were compared to tamoxifen (TAM), 4-hydroxytamoxifen (4-OHT), raloxifene (RAL), 17beta-estradiol (E2) and Diethylstilbestrol (DES). In vitro results indicated that compounds 10 and 12 were the most potent showing significant inhibitory activities against these cell lines. Furthermore, their antiproliferative activity against MCF-7 human breast cancer cell line is comparable to that of TAM, RAL and 4-OHT.
机译:描述了含有碱性氨基侧链的新的基于香豆素的苯并吡喃酮衍生物的合成和抗增殖活性。在20、48、72小时的药物暴露后,使用MTT测定法以0-100μM的浓度确定针对A549和MCF-7人癌细胞的细胞毒性。将这些化合物的抗增殖活性与他莫昔芬(TAM),4-羟基他莫昔芬(4-OHT),雷洛昔芬(RAL),17β-雌二醇(E2)和己烯雌酚(DES)进行了比较。体外结果表明,化合物10和12是最有效的,显示出对这些细胞系的显着抑制活性。此外,它们对MCF-7人乳腺癌细胞系的抗增殖活性与TAM,RAL和4-OHT相当。

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