國家衛生研究院 NHRI:Item 3990099045/8768
English  |  正體中文  |  简体中文  |  全文筆數/總筆數 : 12145/12927 (94%)
造訪人次 : 913085      線上人數 : 1181
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/3990099045/8768


    題名: Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations
    作者: Chen, CT;Hsu, JTA;Lin, WH;Lu, CT;Yen, SC;Hsu, T;Huang, YL;Song, JS;Chen, CH;Chou, LH;Yen, KJ;Chen, CP;Kuo, PC;Huang, CL;Eugene Liu, H;Chao, YS;Yeh, TK;Jiaang, WT
    貢獻者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Numerous FLT3 inhibitors have been explored as a viable therapy for the treatment of acute myeloid leukemia (AML). However, clinical data have been underwhelming due to incomplete inhibition of FLT3 or the emergence of resistant mutations treated with these older agents. We previously developed a series of 3-phenyl-1H-5-pyrazolylamine derivatives as highly potent and selective FLT3 inhibitors with good in vivo efficacy using an intravenous (IV) route. However, the poor bioavailability of these pyrazole compounds limits the development of these promising antileukemic compounds for clinical use. Herein, we describe a novel class of 5-phenyl-thiazol-2-ylamine compounds that are multi-targeted FLT3 inhibitors. From this class of compounds, compound 7h was very potent against AML cell lines and exhibited excellent oral efficacy in AML xenograft models. In addition, further studies demonstrated that compound 7h exhibited potent in vitro and in vivo activities against clinically relevant AC220 (3)-resistant kinase domain mutants of FLT3-ITD.
    日期: 2015-07
    關聯: European Journal of Medicinal Chemistry. 2015 Jul;100:151-161.
    Link to: http://dx.doi.org/10.1016/j.ejmech.2015.05.008
    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:000358097200016
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84931264115
    顯示於類別:[蔣維棠] 期刊論文
    [葉燈光] 期刊論文
    [趙宇生(2002-2013)] 期刊論文
    [徐祖安] 期刊論文
    [陳炯東] 期刊論文

    文件中的檔案:

    檔案 描述 大小格式瀏覽次數
    SDO0223523415300349.pdf1669KbAdobe PDF683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