國家衛生研究院 NHRI:Item 3990099045/7345
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    題名: Exploration of the role of tylophorine E ring in anti-Coronavirus activity-Tylophorine derived dibenzoquinolines impart multi-biological activities as orally active agents
    作者: Lee, YZ;Yang, CW;Hsu, HY;Qiu, YQ;Yeh, TK;Chao, YS;Lee, SJ
    貢獻者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Tylophorine compounds, phenanthroindolizidines and phenanthroquinolizidines, posses multiple potent biological activities including anti-cancer, anti-inflammation, and anti-coronaviruses. In order to explore more classes of tylophorine derivatives for more drug-like compounds, herein we investigate the role of tylophorine E ring in the biological activities through synthesis of a series of compounds with the modification at the E ring either by increasing the C-number or un-cyclizing the E ring and forming different N-substitutes. We have obtained potent derivatives possessing anti-coronavirus activity in terms of anti-TGEV and anti-MHV replication. In addition, the most potent dibenzoquinoline showed improved solubility, in vivo efficacy, and bioavailability as an orally active agent as well as did not showed significant neurotoxicity. The relations of structure and activity of these N-substitutes were analyzed.
    日期: 2013-04-13
    關聯: FASEB Journal. 2013 Apr 13;27:lb71.
    Link to: http://www.fasebj.org/cgi/content/meeting_abstract/27/1_MeetingAbstracts/lb71
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0892-6638&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000319883500410
    顯示於類別:[李秀珠] 會議論文/會議摘要
    [趙宇生(2002-2013)] 會議論文/會議摘要
    [葉燈光] 會議論文/會議摘要

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