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    High-Throughput Screening, Discovery, and Optimization to Develop a Benzofuran Class of Hepatitis C Virus Inhibitors

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    He_2015_HighThroughputScreening.pdf (2.404Mb)
    Issue Date
    2015-09-02
    Author
    He, Shanshan
    Jain, Prashi
    Lin, Billy
    Ferrer, Mark
    Hu, Zongyi
    Southall, Noel
    Hu, Xin
    Zheng, Wei
    Neuenswander, Benjamin
    Cho, Chul-Hee
    Chen, Yu
    Worlikar, Shilpa A.
    Aubé, Jeffrey
    Larock, Richard C.
    Schoenen, Frank J.
    Marugan, Juan J.
    Liang, T. Jake
    Frankowski, Kevin J.
    Publisher
    American Chemical Society
    Type
    Article
    Article Version
    Scholarly/refereed, publisher version
    Metadata
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    Abstract
    Using a high-throughput, cell-based HCV luciferase reporter assay to screen a diverse small-molecule compound collection (~300 000 compounds), we identified a benzofuran compound class of HCV inhibitors. The optimization of the benzofuran scaffold led to the identification of several exemplars with potent inhibition (EC50 < 100 nM) of HCV, low cytotoxicity (CC50 > 25 µM), and excellent selectivity (selective index = CC50/EC50, > 371-fold). The structure–activity studies culminated in the design and synthesis of a 45-compound library to comprehensively explore the anti-HCV activity. The identification, design, synthesis, and biological characterization for this benzofuran series is discussed.
    URI
    http://hdl.handle.net/1808/26723
    DOI
    https://doi.org/10.1021/acscombsci.5b00101
    Collections
    • Chemistry Scholarly Works [553]
    Citation
    Shanshan He, Prashi Jain, Billy Lin, Marc Ferrer, Zongyi Hu, Noel Southall, Xin Hu, Wei Zheng, Benjamin Neuenswander, Chul-Hee Cho, Yu Chen, Shilpa A. Worlikar, Jeffrey Aubé, Richard C. Larock, Frank J. Schoenen, Juan J. Marugan, T. Jake Liang, Kevin J. Frankowski ACS Comb Sci. 2015 Oct 12; 17(10): 641–652. Published online 2015 Sep 17. doi: 10.1021/acscombsci.5b00101

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    KU Libraries
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    785-864-8983

    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
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    Contact KU ScholarWorks
    785-864-8983
    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
    785-864-8983

    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
    Image Credits
     

     

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