國家衛生研究院 NHRI:Item 3990099045/6938
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    题名: Synthesis and biological evaluation of tylophorine-derived dibenzoquinolines as orally active agents: Exploration of the role of tylophorine e ring on biological activity
    作者: Lee, YZ;Yang, CW;Hsu, HY;Qiu, YQ;Yeh, TK;Chang, HY;Chao, YS;Lee, SJ
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: A series of novel tylophorine-derived dibenzoquinolines has been synthesized and their biological activity evaluated. Three assays were conducted: inhibition of cancer cell proliferation, inhibition of TGEV replication for anticoronavirus activity, and suppression of nitric oxide production in RAW264.7 cells (a measure of anti-inflammation). The most potent compound from these assays, dibenzoquinoline 33b, showed improved solubility compared to tylophorine 9a, in vivo efficacies in a lung A549 xenografted tumor mouse model and a murine paw edema model, good bioavailability, and no significant neurotoxicity (as tested by a rota-rod test for motor coordination). This is the first study to explore in detail the role of the tylophorine E ring on biological activity and very strongly suggests that tylophorine-derived dibenzoquinolines merit further development into orally active agents.
    日期: 2012-12-13
    關聯: Journal of Medicinal Chemistry. 2012 Dec 13;55(23):10363-10377.
    Link to: http://dx.doi.org/10.1021/jm300705j
    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:000312227300005
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84871009663
    显示于类别:[葉燈光] 期刊論文
    [李秀珠] 期刊論文
    [趙宇生(2002-2013)] 期刊論文

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