國家衛生研究院 NHRI:Item 3990099045/4939
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    题名: Design and synthesis of alpha-ketoamides as cathepsin S inhibitors with potential applications against tumor invasion and angiogenesis
    其它题名: Design and synthesis of α-ketoamides as cathepsin s inhibitors with potential applications against tumor invasion and angiogenesis
    作者: Chen, JC;Uang, BJ;Lyu, PC;Chang, JY;Liu, KJ;Kuo, CC;Hsieh, HP;Wang, HC;Cheng, CS;Chang, YH;Chang, MDT;Chang, WSW;Lin, CC
    贡献者: National Institute of Cancer Research;Division of Biotechnology and Pharmaceutical Research
    摘要: A series of small molecules bearing an alpha-ketoamide warhead were synthesized and evaluated for their ability to inhibit cathepsin S, a key proteolytic enzyme upregulated in many cancers during tumor progression and metastasis. Most of the synthetic compounds were noncytotoxic, but several robustly inhibited cathepsin S (IC50 < 10 nM) and potently suppressed cell migration, invasion, and capillary tube formation. These results highlight the potential of alpha-ketoamide therapy for preventing or delaying cancer spread.
    日期: 2010-06
    關聯: Journal of Medicinal Chemistry. 2010 Jun;53(11):4545-4549.
    Link to: http://dx.doi.org/10.1021/jm100089e
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0022-2623&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000278298600020
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=77953211174
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