國家衛生研究院 NHRI:Item 3990099045/3977
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    题名: Identification, SAR studies, and X-ray Co-crystallographic analysis of a novel furanopyrimidine aurora kinase a inhibitor
    作者: Coumar, MS;Tsai, MT;Chu, CY;Uang, BJ;Lin, WH;Chang, CY;Chang, TY;Leou, JS;Teng, CH;Wu, JS;Fang, MY;Chen, CH;Hsu, JTA;Wu, SY;Chao, YS;Hsieh, HP
    贡献者: Division of Biotechnology and Pharmaceutical Research
    摘要: Herein we reveal a simple method for the identification of novel Aurora kinase A inhibitors through substructure searching of an in-house compound library to select compounds for testing. A hydrazone fragment conferring Aurora kinase activity and heterocyclic rings most frequently reported in kinase inhibitors were used as substructure queries to filter the in-house compound library collection prior to testing. Five new series of Aurora kinase inhibitors were identified through this strategy, with IC<sub>50</sub> values ranging from ? 300 nm to ? 15 μm, by testing only 133 compounds from a database of ? 125 000 compounds. Structure-activity relationship studies and X-ray co-crystallographic analysis of the most potent compound, a furanopyrimidine derivative with an IC<sub>50</sub> value of 309 nm toward Aurora kinase A, were carried out. The knowledge gained through these studies could help in the future design of potent Aurora kinase inhibitors.
    日期: 2010-02-01
    關聯: ChemMedChem. 2010 Feb 1;5(2):255-267.
    Link to: http://dx.doi.org/10.1002/cmdc.200900339
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=1860-7179&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000274538600010
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=75749152578
    显示于类别:[謝興邦] 期刊論文
    [伍素瑩] 期刊論文
    [徐祖安] 期刊論文
    [趙宇生(2002-2013)] 期刊論文

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