國家衛生研究院 NHRI:Item 3990099045/5506
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    题名: Scaffold-hopping strategy: Synthesis and biological evaluation of 5,6-Fused bicyclic heteroaromatics to identify orally bioavailable anticancer agents
    作者: Tung, YS;Coumar, MS;Wu, YS;Shiao, HY;Chang, JY;Liou, JP;Shukla, P;Chang, CW;Chang, CY;Kuo, CC;Yeh, TK;Lin, CY;Wu, JS;Wu, SY;Liao, CC;Hsieh, HP
    贡献者: Institute of Biotechnology and Pharmaceutical Research;National Institute of Cancer Research
    摘要: Utilizing scaffold-hopping drug-design strategy, we sought to identify a backup drug candidate for BPR0L075 (1), an indole-based anticancer agent. For this purpose, 5,6-fused bicyclic heteroaromatic scaffolds were designed and synthesized through shuffling of the nitrogen from the N-1 position or by insertion of one or two nitrogen atoms into the indole core of 1. Among these, 7-azaindole core 12 showed potent in vitro anticancer activity and improved oral bioavailability (F = 35%) compared with 1 (F < 10%).
    日期: 2011-04-28
    關聯: Journal of Medicinal Chemistry. 2011 Apr 28;54(8):3076-3080.
    Link to: http://dx.doi.org/10.1021/jm101027s
    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:000289697800040
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=79955424472
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