dc.contributor.author | He, Shanshan | |
dc.contributor.author | Jain, Prashi | |
dc.contributor.author | Lin, Billy | |
dc.contributor.author | Ferrer, Mark | |
dc.contributor.author | Hu, Zongyi | |
dc.contributor.author | Southall, Noel | |
dc.contributor.author | Hu, Xin | |
dc.contributor.author | Zheng, Wei | |
dc.contributor.author | Neuenswander, Benjamin | |
dc.contributor.author | Cho, Chul-Hee | |
dc.contributor.author | Chen, Yu | |
dc.contributor.author | Worlikar, Shilpa A. | |
dc.contributor.author | Aubé, Jeffrey | |
dc.contributor.author | Larock, Richard C. | |
dc.contributor.author | Schoenen, Frank J. | |
dc.contributor.author | Marugan, Juan J. | |
dc.contributor.author | Liang, T. Jake | |
dc.contributor.author | Frankowski, Kevin J. | |
dc.date.accessioned | 2018-09-14T17:36:03Z | |
dc.date.available | 2018-09-14T17:36:03Z | |
dc.date.issued | 2015-09-02 | |
dc.identifier.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 | en_US |
dc.identifier.uri | http://hdl.handle.net/1808/26723 | |
dc.description.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. | en_US |
dc.publisher | American Chemical Society | en_US |
dc.subject | Hepatitis C | en_US |
dc.subject | HCV inhibitor | en_US |
dc.subject | Benzofuran | en_US |
dc.subject | Antiviral | en_US |
dc.subject | Hcv replication | en_US |
dc.title | High-Throughput Screening, Discovery, and Optimization to Develop a Benzofuran Class of Hepatitis C Virus Inhibitors | en_US |
dc.type | Article | en_US |
kusw.kuauthor | Neuenswander, Benjamin | |
kusw.kuauthor | Aubé, Jeffrey | |
kusw.kuauthor | Schoenen, Frank J. | |
kusw.kudepartment | Higuchi Biosciences Center | en_US |
kusw.kudepartment | Medicinal Chemistry | en_US |
kusw.kudepartment | Higuchi Biosciences Center | en_US |
dc.identifier.doi | 10.1021/acscombsci.5b00101 | en_US |
kusw.oaversion | Scholarly/refereed, publisher version | en_US |
kusw.oapolicy | This item meets KU Open Access policy criteria. | en_US |
dc.identifier.pmid | PMC6015500 | en_US |
dc.rights.accessrights | openAccess | en_US |