國家衛生研究院 NHRI:Item 3990099045/8104
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    题名: Discovery and structure-activity relationships of phenyl benzenesulfonylhydrazides as novel indoleamine 2,3-dioxygenase inhibitors
    作者: Cheng, MF;Hung, MS;Song, JS;Lin, SY;Liao, FY;Wu, MH;Hsiao, W;Hsieh, CL;Wu, JS;Chao, YS;Shih, C;Wu, SY;Ueng, SH
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: A novel class of phenyl benzenesulfonylhydrazides has been identified as potent inhibitors of indoleamine 2,3-dioxygenase (IDO), and their structure-activity relationship was explored. Coupling reactions between various benzenesulfonyl chlorides and phenylhydrazides were utilized to synthesize the sulfonylhydrazides bearing various substituents. Compound 3i exhibited 61 nM of IC50 in enzymatic assay and 172 nM of EC50 in the HeLa cell. The computational study of 3i suggested that the major interactions between 3i and IDO protein are the coordination of sulfone and heme iron, the hydrogen bonding and hydrophobic interactions between 3i and IDO. This novel class of IDO inhibitor provides a new direction to discover effective anti-cancer agents.
    日期: 2014-08
    關聯: Bioorganic and Medicinal Chemistry Letters. 2014 Aug;24(15):3403-3406.
    Link to: http://dx.doi.org/10.1016/j.bmcl.2014.05.084
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0960-894X&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000339228700037
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84904059888
    显示于类别:[翁紹華] 期刊論文
    [伍素瑩] 期刊論文
    [趙宇生(2002-2013)] 期刊論文
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    [石全(2014-2017)] 期刊論文
    [林書玉] 期刊論文

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