English  |  正體中文  |  简体中文  |  Items with full text/Total items : 12145/12927 (94%)
Visitors : 848975      Online Users : 1477
RC Version 6.0 © Powered By DSPACE, MIT. Enhanced by NTU Library IR team.
Scope Tips:
  • please add "double quotation mark" for query phrases to get precise results
  • please goto advance search for comprehansive author search
    •  Adv. Search
    Home ‧ Login ‧ Upload ‧ Help ‧ About ‧ Administer Goto mobile version


    Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/9549


    Title: Phenyl benzenesulfonylhydrazides exhibit selective Indoleamine 2,3-Dioxygenase inhibition with potent in vivo pharmacodynamic activity and antitumor efficacy
    Authors: 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
    Contributors: Institute of Biotechnology and Pharmaceutical Research
    Abstract: 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.
    Date: 2016-01
    Relation: 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
    Appears in Collections:[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

    Files in This Item:

    File Description SizeFormat
    ISI000368564400029.pdf1232KbAdobe PDF633View/Open


    All items in NHRI are protected by copyright, with all rights reserved.

    Related Items in TAIR

    DSpace Software Copyright © 2002-2004  MIT &  Hewlett-Packard  /   Enhanced by   NTU Library IR team Copyright ©   - Feedback