國家衛生研究院 NHRI:Item 3990099045/8091
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    題名: Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells
    作者: Lee, HY;Tsai, AC;Chen, MC;Shen, PJ;Cheng, YC;Kuo, CC;Pan, SL;Liu, YM;Liu, JF;Yeh, TK;Wang, JC;Chang, CY;Chang, JY;Liou, JP
    貢獻者: National Institute of Cancer Research;Institute of Biotechnology and Pharmaceutical Research
    摘要: A series of indolylsulfonylcinnamic hydroxamates has been synthesized. Compound 12, (E)-3-(3-((1H-pyrrolo[2,3-b]pyridin-1-yl)sulfonyl)phenyl)-N-hydroxyacrylamide, which has a 7-azaindole core cap, was shown to have antiproliferative activity against KB, H460, PC3, HSC-3, HONE-1, A549, MCF-7, TSGH, MKN45, HT29, and HCT116 human cancer cell lines. Pharmacological studies indicated that 12 functions as a potent HDAC inhibitor with an IC50 value of 0.1 mu M. It is highly selective for histone deacetylase 6 (HDAC6) and is 60-fold more active than against HDAC1 and 223-fold more active than against HDAC2. It has a good pharmacokinetic profile with oral bioavailability of 33%. In in vivo efficacy evaluations in colorectal HCT116 xenografts, compound 12 suppresses tumor growth more effectively than SAHA (1, N-hydroxy-N'-phenyloctanediamide) and is therefore seen as a suitable candidate for further investigation.
    日期: 2014-05
    關聯: Journal of Medicinal Chemistry. 2014 May;57(10):4009-4022.
    Link to: http://dx.doi.org/10.1021/jm401899x
    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:000336510100008
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84901263366
    顯示於類別:[張俊彥] 期刊論文
    [葉燈光] 期刊論文
    [郭靜娟] 期刊論文

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