國家衛生研究院 NHRI:Item 3990099045/9549
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    題名: Phenyl benzenesulfonylhydrazides exhibit selective Indoleamine 2,3-Dioxygenase inhibition with potent in vivo pharmacodynamic activity and antitumor efficacy
    作者: Lin, SY;Yeh, TK;Kuo, CC;Song, JS;Cheng, MF;Liao, FY;Chao, MW;Huang, HL;Chen, YL;Yang, CY;Wu, MH;Hsieh, CL;Hsiao, WC;Peng, YH;Wu, JS;Lin, LM;Sun, MW;Chao, YS;Shih, C;Wu, SY;Pan, SL;Hung, MS;Ueng, SH
    貢獻者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Tryptophan metabolism has been recognized as an important mechanism in immune tolerance. Indoleamine 2,3-dioxygenase plays a key role in local tryptophan metabolism via the kynurenine pathway and has emerged as a therapeutic target for cancer immunotherapy. Our prior study identified phenyl benzenesulfonyl hydrazide 2 as a potent in vitro (though not in vivo) inhibitor of indoleamine 2,3-dioxygenase. Further lead optimization to improve in vitro potencies and pharmacokinetic profiles resulted in N'-(4-bromophenyl)-2-oxo-2,3-dihydro-1H-indole-5-sulfonyl hydrazide 40, which demonstrated 59% oral bioavailability and 73% of tumor growth delay without apparent body weight loss in the murine CT26 syngeneic model, after oral administration of 400 mg/kg. Accordingly, 40, is proposed as a potential drug lead worthy of advanced preclinical evaluation.
    日期: 2016-01
    關聯: Journal of Medicinal Chemistry. 2016 Jan;59(1):419-430.
    Link to: http://dx.doi.org/10.1021/acs.jmedchem.5b01640
    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:000368564400029
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84955140232
    顯示於類別:[翁紹華] 期刊論文
    [洪明秀] 期刊論文
    [伍素瑩] 期刊論文
    [石全(2014-2017)] 期刊論文
    [趙宇生(2002-2013)] 期刊論文
    [郭靜娟] 期刊論文
    [葉燈光] 期刊論文
    [林書玉] 期刊論文

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