國家衛生研究院 NHRI:Item 3990099045/4066
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    题名: Anti-influenza drug discovery: structure-activity relationship and mechanistic insight into novel angelicin derivatives
    作者: Yeh, JY;Coumar, MS;Horng, JT;Shiao, HY;Kuo, FM;Lee, HL;Chen, IC;Chang, CW;Tang, WF;Tseng, SN;Chen, CJ;Shih, SR;Hsu, JT;Liao, CC;Chao, YS;Hsieh, HP
    贡献者: Division of Biotechnology and Pharmaceutical Research
    摘要: By using a cell-based high throughput screening campaign, a novel angelicin derivative 6a was identified to inhibit influenza A (H1N1) virus induced cytopathic effect in Madin-Darby canine kidney cell culture in low micromolar range. Detailed structure-activity relationship studies of 6a revealed that the angelicin scaffold is essential for activity in pharmacophore B, while meta-substituted phenyl/2-thiophene rings are optimal in pharmacophore A and C. The optimized lead 4-methyl-9-phenyl-8-(thiophene-2-carbonyl)-furo[2,3-h]chromen-2-one (8g, IC(50) = 70 nM) showed 64-fold enhanced activity compared to the high throughput screening (HTS) hit 6a. Also, 8g was found effective in case of influenza A (H3N2) and influenza B virus strains similar to approved anti-influenza drug zanamivir (4). Preliminary mechanistic studies suggest that these compounds act as anti-influenza agents by inhibiting ribonucleoprotein (RNP) complex associated activity and have the potential to be developed further, which could form the basis for developing additional defense against influenza pandemics.
    日期: 2010-02-25
    關聯: Journal of Medicinal Chemistry. 2010 Feb 25;53(4):1519-1533.
    Link to: http://dx.doi.org/10.1021/jm901570x
    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:000274581200010
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=77649210704
    显示于类别:[謝興邦] 期刊論文
    [趙宇生(2002-2013)] 期刊論文

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