Design, synthesis and biological evaluation of novel furoxan-based coumarin derivatives as antitumor agents

IF 2.6 4区 医学 Q3 CHEMISTRY, MEDICINAL Medicinal Chemistry Research Pub Date : 2018-02-05 DOI:10.1007/s00044-018-2140-x
Zhuo Zhang, Zhi-Wei Bai, Yong Ling, Li-Qin He, Peng Huang, Hong-Xia Gu, Rong-Feng Hu
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引用次数: 29

Abstract

In order to find new anticancer drugs, a series of novel furoxan-based coumarin derivatives (10ak) were synthesized and evaluated for their antiproliferative activities in vitro. All compounds displayed more potent inhibition on human cervical cancer HeLa cell proliferation than coumarin-3-carboxylic acid, and compounds 10b, 10c, 10f, 10h, and 10i with IC50 values ranging from 0.88 to 5.95?μM were even stronger than doxorubicin (IC50?=?10.21?μM). The further study showed that compound 10i exerted the highest antiproliferative activity (IC50?=?0.60?μM) against human breast cancer MCF-7 cells, and compound 10f had broader spectrum antiproliferative activity against five cancer cells with IC50 values in the low micromolar range of 1.86–9.85?μM. More interestingly, compound 10f had little effect on normal intestinal epithelial CCD841 cells. Our findings suggest that these novel furoxan-based coumarin derivatives may provide a new framework for the discovery of novel antitumor agents for the intervention of human carcinoma cells.

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新型呋喃嘧啶类香豆素衍生物抗肿瘤药物的设计、合成及生物学评价
为了寻找新的抗癌药物,合成了一系列新的呋喃嘧啶类香豆素衍生物(10a-k),并对其体外抗增殖活性进行了评价。所有化合物对人宫颈癌HeLa细胞增殖的抑制作用均优于香豆素-3-羧酸和化合物10b、10c、10f、10h和10i, IC50值在0.88 ~ 5.95?μM比阿霉素更强(IC50 = 10.21 μM)。进一步研究表明,化合物10i对人乳腺癌MCF-7细胞的抑制活性最高(IC50 = 0.60 μM),化合物10f对5种肿瘤细胞的抑制活性谱较宽,IC50值在1.86 ~ 9.85 μM的低微摩尔范围内。更有趣的是,化合物10f对正常肠上皮CCD841细胞几乎没有影响。我们的研究结果表明,这些新的呋喃嘧啶类香豆素衍生物可能为发现新的抗肿瘤药物干预人类癌细胞提供一个新的框架。
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来源期刊
Medicinal Chemistry Research
Medicinal Chemistry Research 医学-医药化学
CiteScore
4.70
自引率
3.80%
发文量
162
审稿时长
5.0 months
期刊介绍: Medicinal Chemistry Research (MCRE) publishes papers on a wide range of topics, favoring research with significant, new, and up-to-date information. Although the journal has a demanding peer review process, MCRE still boasts rapid publication, due in part, to the length of the submissions. The journal publishes significant research on various topics, many of which emphasize the structure-activity relationships of molecular biology.
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