國家衛生研究院 NHRI:Item 3990099045/9926
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    题名: Discovery of novel inhibitors of Aurora kinases with indazole scaffold: In silico fragment-based and knowledge-based drug design
    作者: Chang, CF;Lin, WH;Ke, YY;Lin, YS;Wang, WC;Chen, CH;Kuo, PC;Hsu, JTA;Uang, BJ;Hsieh, HP
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Aurora kinases have emerged as important anticancer targets so that there are several inhibitors have advanced into clinical study. Herein, we identified novel indazole derivatives as potent Aurora kinases inhibitors by utilizing in silico fragment-based approach and knowledge-based drug design. After intensive hit-to-lead optimization, compounds 17 (dual Aurora A and B), 21 (Aurora B selective) and 30 (Aurora A selective) possessed indazole privileged scaffold with different substituents, which provide sub-type kinase selectivity. Computational modeling helps in understanding that the isoform selectivity could be targeted specific residue in the Aurora kinase binding pocket in particular targeting residues Arg220, Thr217 or Glu177.
    日期: 2016-11-29
    關聯: European Journal of Medicinal Chemistry. 2016 Nov 29;124:186-199.
    Link to: http://dx.doi.org/10.1016/j.ejmech.2016.08.026
    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:000388544600014
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84983638191
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