國家衛生研究院 NHRI:Item 3990099045/9540
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    题名: Synthesis and evaluation of aminothiazole-paeonol derivatives as potential anticancer agents
    作者: Tsai, CY;Kapoor, M;Huang, YP;Lin, HH;Liang, YC;Lin, YL;Huang, SC;Liao, WN;Chen, JK;Huang, JS;Hsu, MH
    贡献者: Institute of Biomedical Engineering and Nanomedicine
    摘要: In this study, novel aminothiazole-paeonol derivatives were synthesized and characterized using (1)H-NMR, (13)C-NMR, IR, mass spectroscopy, and high performance liquid chromatography. All the new synthesized compounds were evaluated according to their anticancer effect on seven cancer cell lines. The experimental results indicated that these compounds possess high anticancer potential regarding human gastric adenocarcinoma (AGS cells) and human colorectal adenocarcinoma (HT-29 cells). Among these compounds, N-[4-(2-hydroxy-4-methoxyphenyl)thiazol-2-yl]-4-methoxybenzenesulfonamide (13c) had the most potent inhibitory activity, with IC50 values of 4.0 microM to AGS, 4.4 microM to HT-29 cells and 5.8 microM to HeLa cells. The 4-fluoro-N-[4-(2-hydroxy-4-methoxyphenyl)thiazol-2-yl]benzenesulfonamide (13d) was the second potent compound, showing IC50 values of 7.2, 11.2 and 13.8 microM to AGS , HT-29 and HeLa cells, respectively. These compounds are superior to 5-fluorouracil (5-FU) for relatively higher potency against AGS and HT-29 human cancer cell lines along with lower cytotoxicity to fibroblasts. Novel aminothiazole-paeonol derivatives in this work might be a series of promising lead compounds to develop anticancer agents for treating gastrointestinal adenocarcinoma.
    日期: 2016-01
    關聯: Molecules. 2016 Jan;21(2):Article number E145.
    Link to: http://dx.doi.org/10.3390/molecules21020145
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=1420-3049&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000371895900034
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84964573683
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