English  |  正體中文  |  简体中文  |  全文筆數/總筆數 : 12500/13673 (91%)
造訪人次 : 2477102      線上人數 : 62
RC Version 6.0 © Powered By DSPACE, MIT. Enhanced by NTU Library IR team.
搜尋範圍 查詢小技巧：
  • 您可在西文檢索詞彙前後加上"雙引號"，以獲取較精準的檢索結果
  • 若欲以作者姓名搜尋，建議至進階搜尋限定作者欄位，可獲得較完整資料
    •  進階搜尋
    主頁 ‧ 登入 ‧ 上傳 ‧ 說明 ‧ 關於NHRI ‧ 管理 到手機版


    請使用永久網址來引用或連結此文件: http://ir.nhri.org.tw/handle/3990099045/13875


    題名: Discovery and development of a novel N-(3-bromophenyl)-{[(phenylcarbamoyl)amino]methyl}-N-hydroxythiophene-2-carboximidamide indoleamine 2,3-dioxygenase inhibitor using knowledge-based drug design
    作者: Yeh, TK;Song, JS;Chang, PW;Yu, JC;Chang, CH;Liao, FY;Tien, YW;Kuppusamy, R;Li, AS;Chen, CH;Chen, CW;Lin, LM;Chang, HH;Huang, CH;Yao, JY;Wu, MH;Peng, YH;Hsueh, CC;Hsiao, WC;Chen, PH;Lin, CY;Hsieh, SH;Shih, C;Hung, MS;Wu, SY;Kuo, CC;Ueng, SH
    貢獻者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Indoleamine 2,3-dioxygenase-1 (IDO1) is a potential target for the next generation of cancer immunotherapies. We describe the development of two series of IDO1 inhibitors incorporating a N-hydroxy-thiophene-carboximidamide core generated by knowledge-based drug design. Structural modifications to improve the cellular activity and pharmacokinetic (PK) properties of the compounds synthesized, including extension of the side chain of the N-hydroxythiophene-2-carboximidamide core, resulted in compound 27a, a potent IDO1 inhibitor which demonstrated significant (51%) in vivo target inhibition on IDO1 in a human SK-OV-3 ovarian xenograft tumor mouse model. This strategy is expected to be applicable to the discovery of additional IDO1 inhibitors for the treatment of other diseases susceptible to modulation of IDO1.
    日期: 2022-02-05
    關聯: European Journal of Medicinal Chemistry. 2022 Feb 5;229:Article number 114043.
    Link to: http://dx.doi.org/10.1016/j.ejmech.2021.114043
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0223-5234&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000766121600003
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85121273827
    顯示於類別:[翁紹華] 期刊論文
    [郭靜娟] 期刊論文
    [伍素瑩] 期刊論文
    [洪明秀] 期刊論文
    [石全(2014-2017)] 期刊論文
    [葉燈光] 期刊論文

    文件中的檔案:

    檔案 描述 大小格式瀏覽次數
    SCP85121273827.pdf2042KbAdobe PDF261檢視/開啟


    在NHRI中所有的資料項目都受到原著作權保護.

    TAIR相關文章

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