國家衛生研究院 NHRI:Item 3990099045/3975
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    Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/3975


    Title: Identification of benzofuro[2,3-b]quinoline derivatives as a new class of antituberculosis agents
    Authors: Yang, CL;Tseng, CH;Chen, YL;Lu, CM;Kao, CL;Wu, MH;Tzeng, CC
    Contributors: Division of Biotechnology and Pharmaceutical Research
    Abstract: A series of 11-alkoxylated and 11-aminated benzofuro[2,3-b]quinoline derivatives were designed, synthesized, and evaluated for their anti-TB and cytotoxic activities. The known 11-chlorobenzofuro[2,3-b]quinoline (3) was synthesized in a single step from anthranilic acid and 2-coumaranone in phosphorus oxychloride in 51% yield for the first time. Treatment of 3 with alcohols and amines gave 11-alkoxylated and 11-aminated benzofuro[2,3-b]quinoline derivatives respectively, which were evaluated for their anti-TB and cytotoxic activities. Our results indicated that 11-arylaminated derivatives were more active than their respective 11-aryloxylated isosteric isomers against Mycobacterium tuberculosis. Among the tested compounds, 11-methoxybenzofuro[2,3-b]quinoline (4), 11-methylamino- benzofuro[2,3-b]quinoline (9), and 11-dimethylaminobenzofuro[2,3-b]quinoline (14) exhibited significant activities against the growth of M. tuberculosis (MIC values of <0.20 μg/mL) and low cytotoxicities against VERO cell with IC<sub>50</sub> values of 11.77, 5.55, and >30.00 μg/mL respectively. The selectivity index (SI = IC<sub>50</sub>/MIC) for 4, 9, and 14 was greater than 58.85, 27.75, and 150 respectively.
    Date: 2010-02
    Relation: European Journal of Medicinal Chemistry. 2010 Feb;45(2):602-607.
    Link to: http://dx.doi.org/10.1016/j.ejmech.2009.10.050
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0223-5234&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000274773300023
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=73549088732
    Appears in Collections:[Others] Periodical Articles

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