國家衛生研究院 NHRI:Item 3990099045/8335
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    题名: 1-Arylsulfonyl-5-(N-hydroxyacrylamide)tetrahydroquinolines as potent histone deacetylase inhibitors suppressing the growth of prostate cancer cells
    作者: Liu, YM;Lee, HY;Chen, CH;Lee, CH;Wang, LT;Pan, SL;Lai, MJ;Yeh, TK;Liou, JP
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: This study describes the development of a series of 1-arylsulfonyl-6- (N-hydroxyacrylamide)tetrahydroquinolines, potent histone deacetylase (HDAC) inhibitors which are cytotoxic to PC-3 cells. (E)-N-hydroxy-3-(1-(4-methoxyphenylsulfonyl)-1,2,3,4- tetrahydroquinolin-6-yl)acrylamide (11) exhibits marked anti-HDAC and antiproliferative activity, and is slightly more effective than N1-hydroxy-N8-phenyloctanediamide (SAHA, Vorinostat, 1). In a xenograft tumor model, 11, at doses of 100 or 200 mg/kg orally, suppresses the growth of PC-3 cells and leads to tumor growth inhibition of 38.8% and 57.9%, respectively. Compound 11 is a lead compound for further development of potential prostate cancer inhibitors.
    日期: 2015-01
    關聯: European Journal of Medicinal Chemistry. 2015 Jan;89:320-330.
    Link to: http://dx.doi.org/10.1016/j.ejmech.2014.10.052
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0223-5234&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000348003500029
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84908277134
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