國家衛生研究院 NHRI:Item 3990099045/1152
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    jsp.display-item.identifier=請使用永久網址來引用或連結此文件: http://ir.nhri.org.tw/handle/3990099045/1152


    题名: Design, synthesis, and structure-activity relationships of pyrazolo[3,4-d]pyrimidinies: a novel class of potent enterovirus inhibitors
    其它题名: Design, synthesis, and struc-ture-activity relationships of pyrazolo[3,4-d]pyrimidinies: a novel class of potent enterovirus inhibitors
    作者: Chern, JH;Shia, KS;Hsu, TA;Tai, CL;Lee, CC;Lee, YC;Chang, CS;Tseng, SN;Shih, SR
    贡献者: Division of Biotechnology and Pharmaceutical Research
    摘要: A series of pyrazolo[3,4-d]pyrimidines were synthesized. and their antiviral activity was evaluated in a plaque reduction assay. It is very interesting that this class of compounds provide remarkable evidence that they are very specific for human enteroviruses, in particular, coxsackieviruses. Some derivatives proved to be highly effective in inhibiting enterovirus replication at nanomolar concentrations. SAR studies revealed that the phenyl group at the N-I position and the hydrophobic diarylmethyl group at the piperazine largely influenced the in vitro antienteroviral activity of this new class of potent antiviral agents. It was found that the pyrazolo[3,4-d]pyrimidines with a thiophene substituent, such as compounds 20 24, in general exhibited high activity against coxsackievirus B3 (IC50 = 0.063-0.089 muM) and moderate activity against enterovirus 71 (IC50 = 0.32-0.65 muM) with no apparent cytotoxic effect toward RD (rhabdomyosarcoma) cell lines (CC50>25 muM). (C) 2004 Elsevier Ltd. All rights reserved.
    关键词: Chemistry, Medicinal;Chemistry, Organic
    日期: 2004-05-17
    關聯: Bioorganic and Medicinal Chemistry Letters. 2004 May;14(10):2519-2525.
    Link to: http://dx.doi.org/10.1016/j.bmcl.2004.02.092
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0960-894X&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000221316000025
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=1942438497
    显示于类别:[徐祖安] 期刊論文
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