Compound Aggregation in Drug Discovery: Implementing a Practical NMR Assay for Medicinal Chemists
LaPlante, Steven R, Carson, Rebekah, Gillard, James, Aubry, Norman, Coulombe, René, Bordeleau, Sylvain, Bonneau, Pierre, Little, Michael, O’Meara, Jeff, Beaulieu, Pierre L
Published in Journal of medicinal chemistry (27.06.2013)
Published in Journal of medicinal chemistry (27.06.2013)
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Monitoring Drug Self-Aggregation and Potential for Promiscuity in Off-Target In Vitro Pharmacology Screens by a Practical NMR Strategy
LaPlante, Steven R, Aubry, Norman, Bolger, Gordon, Bonneau, Pierre, Carson, Rebekah, Coulombe, René, Sturino, Claudio, Beaulieu, Pierre L
Published in Journal of medicinal chemistry (12.09.2013)
Published in Journal of medicinal chemistry (12.09.2013)
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Journal Article
Enantiomeric Atropisomers Inhibit HCV Polymerase and/or HIV Matrix: Characterizing Hindered Bond Rotations and Target Selectivity
LaPlante, Steven R., Forgione, Pat, Boucher, Colette, Coulombe, René, Gillard, James, Hucke, Oliver, Jakalian, Araz, Joly, Marc-André, Kukolj, George, Lemke, Christopher, McCollum, Robert, Titolo, Steve, Beaulieu, Pierre L., Stammers, Timothy
Published in Journal of medicinal chemistry (13.03.2014)
Published in Journal of medicinal chemistry (13.03.2014)
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Binding Site Characterization and Resistance to a Class of Non-nucleoside Inhibitors of the Hepatitis C Virus NS5B Polymerase
Kukolj, George, McGibbon, Graham A., McKercher, Ginette, Marquis, Martin, Lefèbvre, Sylvain, Thauvette, Louise, Gauthier, Jean, Goulet, Sylvie, Poupart, Marc-André, Beaulieu, Pierre L.
Published in The Journal of biological chemistry (25.11.2005)
Published in The Journal of biological chemistry (25.11.2005)
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Journal Article
Non-Nucleoside Benzimidazole-Based Allosteric Inhibitors of the Hepatitis C Virus NS5B Polymerase: Inhibition of Subgenomic Hepatitis C Virus RNA Replicons in Huh-7 Cells
Beaulieu, Pierre L, Bousquet, Yves, Gauthier, Jean, Gillard, James, Marquis, Martin, McKercher, Ginette, Pellerin, Charles, Valois, Serge, Kukolj, George
Published in Journal of medicinal chemistry (30.12.2004)
Published in Journal of medicinal chemistry (30.12.2004)
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Journal Article
Improved replicon cellular activity of non-nucleoside allosteric inhibitors of HCV NS5B polymerase: From benzimidazole to indole scaffolds
Beaulieu, Pierre L., Gillard, James, Bykowski, Darren, Brochu, Christian, Dansereau, Nathalie, Duceppe, Jean-Simon, Haché, Bruno, Jakalian, Araz, Lagacé, Lisette, LaPlante, Steven, McKercher, Ginette, Moreau, Elaine, Perreault, Stéphane, Stammers, Timothy, Thauvette, Louise, Warrington, Jeff, Kukolj, George
Published in Bioorganic & medicinal chemistry letters (01.10.2006)
Published in Bioorganic & medicinal chemistry letters (01.10.2006)
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Synthesis of (1R,2S)-1-Amino-2-vinylcyclopropanecarboxylic Acid Vinyl-ACCA) Derivatives: Key Intermediates for the Preparation of Inhibitors of the Hepatitis C Virus NS3 Protease
Beaulieu, Pierre L, Gillard, James, Bailey, Murray D, Boucher, Colette, Duceppe, Jean-Simon, Simoneau, Bruno, Wang, Xiao-Jun, Zhang, Li, Grozinger, Karl, Houpis, Ioannis, Farina, Vittorio, Heimroth, Heidi, Krueger, Thomas, Schnaubelt, Jürgen
Published in Journal of organic chemistry (22.07.2005)
Published in Journal of organic chemistry (22.07.2005)
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Journal Article
Aza follow-ups to BI 207524, a thumb pocket 1 HCV NS5B polymerase inhibitor. Part 1: Mitigating the genotoxic liability of an aniline metabolite
Beaulieu, Pierre L., Bolger, Gordon, Duplessis, Martin, Gagnon, Alexandre, Garneau, Michel, Stammers, Timothy, Kukolj, George, Duan, Jianmin
Published in Bioorganic & medicinal chemistry letters (01.03.2015)
Published in Bioorganic & medicinal chemistry letters (01.03.2015)
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Conformation-Based Restrictions and Scaffold Replacements in the Design of Hepatitis C Virus Polymerase Inhibitors: Discovery of Deleobuvir (BI 207127)
LaPlante, Steven R., Bös, Michael, Brochu, Christian, Chabot, Catherine, Coulombe, René, Gillard, James R., Jakalian, Araz, Poirier, Martin, Rancourt, Jean, Stammers, Timothy, Thavonekham, Bounkham, Beaulieu, Pierre L., Kukolj, George, Tsantrizos, Youla S.
Published in Journal of medicinal chemistry (13.03.2014)
Published in Journal of medicinal chemistry (13.03.2014)
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A prodrug strategy for the oral delivery of a poorly soluble HCV NS5B thumb pocket 1 polymerase inhibitor using self-emulsifying drug delivery systems (SEDDS)
Beaulieu, Pierre L., De Marte, Josie, Garneau, Michel, Luo, Laibin, Stammers, Timothy, Telang, Chitra, Wernic, Dominik, Kukolj, George, Duan, Jianmin
Published in Bioorganic & medicinal chemistry letters (15.01.2015)
Published in Bioorganic & medicinal chemistry letters (15.01.2015)
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Journal Article
Discovery of the First Thumb Pocket 1 NS5B Polymerase Inhibitor (BILB 1941) with Demonstrated Antiviral Activity in Patients Chronically Infected with Genotype 1 Hepatitis C Virus (HCV)
Beaulieu, Pierre L, Bös, Michael, Cordingley, Michael G, Chabot, Catherine, Fazal, Gulrez, Garneau, Michel, Gillard, James R, Jolicoeur, Eric, LaPlante, Steven, McKercher, Ginette, Poirier, Martin, Poupart, Marc-André, Tsantrizos, Youla S, Duan, Jianmin, Kukolj, George
Published in Journal of medicinal chemistry (13.09.2012)
Published in Journal of medicinal chemistry (13.09.2012)
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Journal Article
Multi-parameter optimization of aza-follow-ups to BI 207524, a thumb pocket 1 HCV NS5B polymerase inhibitor. Part 2: Impact of lipophilicity on promiscuity and in vivo toxicity
Beaulieu, Pierre L., Bolger, Gordon, Deon, Dan, Duplessis, Martin, Fazal, Gulrez, Gagnon, Alexandre, Garneau, Michel, LaPlante, Steven, Stammers, Timothy, Kukolj, George, Duan, Jianmin
Published in Bioorganic & medicinal chemistry letters (01.03.2015)
Published in Bioorganic & medicinal chemistry letters (01.03.2015)
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Journal Article
Importance of Ligand Bioactive Conformation in the Discovery of Potent Indole-Diamide Inhibitors of the Hepatitis C Virus NS5B
LaPlante, Steven R, Gillard, James R, Jakalian, Araz, Aubry, Norman, Coulombe, René, Brochu, Christian, Tsantrizos, Youla S, Poirier, Martin, Kukolj, George, Beaulieu, Pierre L
Published in Journal of the American Chemical Society (03.11.2010)
Published in Journal of the American Chemical Society (03.11.2010)
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Journal Article
Molecular Dynamics Simulations and Structure-Based Rational Design Lead to Allosteric HCV NS5B Polymerase Thumb Pocket 2 Inhibitor with Picomolar Cellular Replicon Potency
Hucke, Oliver, Coulombe, René, Bonneau, Pierre, Bertrand-Laperle, Mégan, Brochu, Christian, Gillard, James, Joly, Marc-André, Landry, Serge, Lepage, Olivier, Llinàs-Brunet, Montse, Pesant, Marc, Poirier, Martin, Poirier, Maude, McKercher, Ginette, Marquis, Martin, Kukolj, George, Beaulieu, Pierre L., Stammers, Timothy A.
Published in Journal of medicinal chemistry (13.03.2014)
Published in Journal of medicinal chemistry (13.03.2014)
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Journal Article
From benzimidazole to indole-5-carboxamide Thumb Pocket I inhibitors of HCV NS5B polymerase. Part 1: Indole C-2 SAR and discovery of diamide derivatives with nanomolar potency in cell-based subgenomic replicons
Beaulieu, Pierre L., Gillard, James, Jolicoeur, Eric, Duan, Jianmin, Garneau, Michel, Kukolj, George, Poupart, Marc-André
Published in Bioorganic & medicinal chemistry letters (15.06.2011)
Published in Bioorganic & medicinal chemistry letters (15.06.2011)
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Journal Article
Discovery of BI 207524, an Indole Diamide NS5B Thumb Pocket 1 Inhibitor with Improved Potency for the Potential Treatment of Chronic Hepatitis C Virus Infection
Beaulieu, Pierre L, Anderson, Paul C, Bethell, Richard, Bös, Michael, Bousquet, Yves, Brochu, Christian, Cordingley, Michael G, Fazal, Gulrez, Garneau, Michel, Gillard, James R, Kawai, Stephen, Marquis, Martin, McKercher, Ginette, Poupart, Marc-André, Stammers, Timothy, Thavonekham, Bounkham, Wernic, Dominik, Duan, Jianmin, Kukolj, George
Published in Journal of medicinal chemistry (11.12.2014)
Published in Journal of medicinal chemistry (11.12.2014)
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