國家衛生研究院 NHRI:Item 3990099045/11078
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    题名: 4-Bromophenylhydrazinyl benzenesulfonylphenylureas as indoleamine 2,3-dioxygenase inhibitors with in vivo target inhibition and anti-tumor efficacy
    作者: Lin, SY;Yeh, TK;Song, JS;Hung, MS;Cheng, MF;Liao, FY;Li, AS;Cheng, SY;Lin, LM;Chiu, CH;Wu, MH;Lin, YJ;Hsiao, W;Sun, M;Wang, YH;Huang, CH;Tang, YC;Chang, HH;Huang, ZT;Chao, YS;Shih, C;Pan, SL;Wu, SY;Kuo, CC;Ueng, SH
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Indoleamine 2,3-dioxygenase is a heme-containing enzyme implicated in the down regulation of the anti-tumor immune response, and considered a promising anti-cancer drug target. Several pharmaceutical companies, including Pfizer, Merck, and Bristol-Myers Squibb, are known to be in pursuit of IDO inhibitors, and Incyte recently reported good results in the phase II clinical trial of the IDO inhibitor Epacadostat. In previous work, we developed a series of IDO inhibitors based on a sulfonylhydrazide core structure, and explored how they could serve as potent IDO inhibitors with good drug profiles. Herein, we disclose the development of the 4-bromophenylhydrazinyl benzenesulfonylphenylurea 5k, a potent IDO inhibitor which demonstrated 25% tumor growth inhibition in a murine CT26 syngeneic model on day 18 with 100 mg/kg oral administration twice daily, and a 30% reduction in tumor weight. Pharmacodynamic testing of 5k found it to cause a 25% and 21% reduction in kyn/trp ratio at the plasma and tumor, respectively. In the CT26 tumor model, 5k was found to slightly increase the percentage of CD3+ T cells and lymphocyte responsiveness, indicating that 5k may have potential in modulating anti-tumor immunity. These data suggest 5k to be worthy of further investigation in the development of anti-tumor drugs.
    日期: 2018-04
    關聯: Bioorganic Chemistry. 2018 Apr;77:600-607.
    Link to: http://dx.doi.org/10.1016/j.bioorg.2018.02.010
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0045-2068&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000428013300064
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85042508065
    显示于类别:[翁紹華] 期刊論文
    [郭靜娟] 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
    [洪明秀] 期刊論文
    [葉燈光] 期刊論文
    [林書玉] 期刊論文

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