{"title":"Design, synthesis and biological evaluation of novel furoxan-based coumarin derivatives as antitumor agents","authors":"Zhuo Zhang, Zhi-Wei Bai, Yong Ling, Li-Qin He, Peng Huang, Hong-Xia Gu, Rong-Feng Hu","doi":"10.1007/s00044-018-2140-x","DOIUrl":null,"url":null,"abstract":"<p>In order to find new anticancer drugs, a series of novel furoxan-based coumarin derivatives (<b>10a</b>–<b>k</b>) 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 <b>10b</b>,<b> 10c</b>,<b> 10f</b>,<b> 10h</b>, and <b>10i</b> with IC<sub>50</sub> values ranging from 0.88 to 5.95?μM were even stronger than doxorubicin (IC<sub>50</sub>?=?10.21?μM). The further study showed that compound <b>10i</b> exerted the highest antiproliferative activity (IC<sub>50</sub>?=?0.60?μM) against human breast cancer MCF-7 cells, and compound <b>10f</b> had broader spectrum antiproliferative activity against five cancer cells with IC<sub>50</sub> values in the low micromolar range of 1.86–9.85?μM. More interestingly, compound <b>10f</b> 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.</p>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"27 4","pages":"1198 - 1205"},"PeriodicalIF":2.6000,"publicationDate":"2018-02-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1007/s00044-018-2140-x","citationCount":"29","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Medicinal Chemistry Research","FirstCategoryId":"3","ListUrlMain":"https://link.springer.com/article/10.1007/s00044-018-2140-x","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 29
Abstract
In order to find new anticancer drugs, a series of novel furoxan-based coumarin derivatives (10a–k) 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.
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.