國家衛生研究院 NHRI:Item 3990099045/8768
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    题名: 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
    贡献者: 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
    显示于类别:[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

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