國家衛生研究院 NHRI:Item 3990099045/9423
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    題名: 2-Aroylquinoline-5,8-diones as potent anticancer agents displaying tubulin and heat shock protein 90 (HSP90) inhibition
    作者: Nepali, K;Kumar, S;Huang, HL;Kuo, FC;Lee, CH;Kuo, CC;Yeh, TK;Li, YH;Chang, JY;Liou, JP;Lee, HY
    貢獻者: National Institute of Cancer Research;Institute of Biotechnology and Pharmaceutical Research
    摘要: This study reports the synthesis of a series of 2-aroylquinoline-5,8-diones (11-23) on the basis of scaffold hopping. The presence of a methoxy group at C6 assists the highly regioselective incorporation with various amines, and simplifies the structural identification process. Among the synthetic compounds, 6-dimethylamino-2-(3,4,5-trimethoxybenzoyl)-quinoline-5,8-dione (12) and 7-pyrrolidin-1-yl-2-(3,4,5-trimethoxybenzoyl)-quinoline-5,8-dione (23) exhibit remarkable anti-proliferative activity against the cancer cell lines tested with mean IC50 values of 0.14 and 0.27 [small mu ]M, respectively. Compound 23 showed moderate inhibitory activity against tubulin polymerization with an IC50 value of 5.9 [small mu ]M. In a western blot analysis, 23 caused induction of HSP70 and degradation of Akt, revealing that it possesses HSP90 inhibitory activity.
    日期: 2016-01
    關聯: Organic and Biomolecular Chemistry. 2016 Jan;14(2):716-723.
    Link to: http://dx.doi.org/10.1039/C5OB02100F
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=1477-0520&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000367343800029
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84953297826
    顯示於類別:[張俊彥] 期刊論文
    [葉燈光] 期刊論文
    [郭靜娟] 期刊論文

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