國家衛生研究院 NHRI:Item 3990099045/5790
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    题名: Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3)
    作者: Lin, WH;Hsieh, SY;Yen, SC;Chen, CT;Yeh, TK;Hsu, T;Lu, CT;Chen, CP;Chen, CW;Chou, LH;Huang, YL;Cheng, AH;Chang, YI;Tseng, YJ;Yen, KR;Chao, YS;Hsu, JT;Jiaang, WT
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Preclinical investigations and early clinical trial studies suggest that FLT3 inhibitors offer a viable therapy for acute myeloid leukemia. However, early clinical data for direct FLT3 inhibitors provided only modest results because of the failure to fully inhibit FLT3. We have designed and synthesized a novel class of 3-phenyl-1H-5-pyrazolylamine-derived compounds as FLT3 inhibitors which exhibit potent FLT3 inhibition and high selectivity toward different receptor tyrosine kinases. The structure-activity relationships led to the discovery of two series of FLT3 inhibitors, and some potent compounds within these two series exhibited comparable potency to FLT3 inhibitors sorafenib (3) and ABT-869 (4) in both wt-FLT3 enzyme inhibition and FLT3-ITD inhibition on cell growth (MOLM-13 and MV4;11 cells). In particular, the selected compound 12a exhibited the ability to regress tumors in mouse xenograft models using MOLM-13 and MV4;11 cells.
    日期: 2011-07
    關聯: Bioorganic and Medicinal Chemistry. 2011 Jul;19(14):4173-4182 .
    Link to: http://dx.doi.org/10.1016/j.bmc.2011.06.016
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0968-0896&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000292301200002
    https://www.webofscience.com/wos/woscc/full-record/WOS:000292301200002
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=79959956358
    显示于类别:[蔣維棠] 期刊論文
    [徐祖安] 期刊論文
    [趙宇生(2002-2013)] 期刊論文
    [葉燈光] 期刊論文
    [陳炯東] 期刊論文

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