國家衛生研究院 NHRI:Item 3990099045/6420
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    題名: Synthesis and biological evaluation of 1-Arylsulfonyl-5-(N-hydroxyacrylamide)indoles as potent histone deacetylase inhibitors with antitumor activity in vivo
    作者: Lai, MJ;Huang, HL;Pan, SL;Liu, YM;Peng, CY;Lee, HY;Yeh, TK;Huang, PH;Teng, CM;Chen, CS;Chuang, HY;Liou, JP
    貢獻者: Institute of Biotechnology and Pharmaceutical Research
    摘要: A series of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles has been identified as a new class of histone deacetylase inhibitors. Compounds 8, 11, 12, 13, and 14 demonstrated stronger antiproliferative activities than 1 (SAHA) with GI(50) values ranging from 0.36 to 1.21 mu M against Hep3B, MDA-MB-231, PC-3, and A549 human cancer cell lines. Lead compound 8 showed remarkable HDAC 1, 2, and 6 isoenzymes inhibitory activities with IC50 values of 12.3, 4.0, 1.0 nM, respectively, which are comparable to I. In in vivo efficacy evaluation against lung A549 xenograft model, 8 displayed better antitumor activity than compound 1.
    日期: 2012-04
    關聯: Journal of Medicinal Chemistry. 2012 Apr;55(8):3777-3791.
    Link to: http://dx.doi.org/10.1021/jm300197a
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0022-2623&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000303173600013
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84860312887
    顯示於類別:[葉燈光] 期刊論文
    [潘秀玲(2009-2013)] 期刊論文

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