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dc.contributor.authorYeh, Jiann-Yihen_US
dc.contributor.authorCoumar, Mohane Selvarajen_US
dc.contributor.authorHorng, Jim-Tongen_US
dc.contributor.authorShiao, Hui-Yien_US
dc.contributor.authorKuo, Fu-Mingen_US
dc.contributor.authorLee, Hui-Lingen_US
dc.contributor.authorChen, In-Chunen_US
dc.contributor.authorChang, Chun-Weien_US
dc.contributor.authorTang, Wen-Fangen_US
dc.contributor.authorTseng, Sung-Nainen_US
dc.contributor.authorChen, Chi-Jeneen_US
dc.contributor.authorShih, Shin-Ruen_US
dc.contributor.authorHsu, John T. -Aen_US
dc.contributor.authorLiao, Chun-Chenen_US
dc.contributor.authorChao, Yu-Shengen_US
dc.contributor.authorHsieh, Hsing-Pangen_US
dc.date.accessioned2014-12-08T15:07:23Z-
dc.date.available2014-12-08T15:07:23Z-
dc.date.issued2010-02-25en_US
dc.identifier.issn0022-2623en_US
dc.identifier.urihttp://dx.doi.org/10.1021/jm901570xen_US
dc.identifier.urihttp://hdl.handle.net/11536/5821-
dc.description.abstractBy 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 ill 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.en_US
dc.language.isoen_USen_US
dc.titleAnti-Influenza Drug Discovery: Structure-Activity Relationship and Mechanistic Insight into Novel Angelicin Derivativesen_US
dc.typeArticleen_US
dc.identifier.doi10.1021/jm901570xen_US
dc.identifier.journalJOURNAL OF MEDICINAL CHEMISTRYen_US
dc.citation.volume53en_US
dc.citation.issue4en_US
dc.citation.spage1519en_US
dc.citation.epage1533en_US
dc.contributor.department生物科技學系zh_TW
dc.contributor.departmentDepartment of Biological Science and Technologyen_US
dc.identifier.wosnumberWOS:000274581200010-
dc.citation.woscount30-
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