Anthranilic acid-based Thumb Pocket 2 HCV NS5B polymerase inhibitors with sub-micromolar potency in the cell-based replicon assay
Stammers, Timothy A., Coulombe, René, Duplessis, Martin, Fazal, Gulrez, Gagnon, Alexandre, Garneau, Michel, Goulet, Sylvie, Jakalian, Araz, LaPlante, Steven, Rancourt, Jean, Thavonekham, Bounkham, Wernic, Dominik, Kukolj, George, Beaulieu, Pierre L.
Published in Bioorganic & medicinal chemistry letters (15.12.2013)
Published in Bioorganic & medicinal chemistry letters (15.12.2013)
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Journal Article
Structure-based design of novel HCV NS5B thumb pocket 2 allosteric inhibitors with submicromolar gt1 replicon potency: Discovery of a quinazolinone chemotype
Beaulieu, Pierre L., Coulombe, René, Duan, Jianmin, Fazal, Gulrez, Godbout, Cédrickx, Hucke, Oliver, Jakalian, Araz, Joly, Marc-André, Lepage, Olivier, Llinàs-Brunet, Montse, Naud, Julie, Poirier, Martin, Rioux, Nathalie, Thavonekham, Bounkham, Kukolj, George, Stammers, Timothy A.
Published in Bioorganic & medicinal chemistry letters (15.07.2013)
Published in Bioorganic & medicinal chemistry letters (15.07.2013)
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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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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
Discovery of a novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors
Stammers, Timothy A., Coulombe, René, Rancourt, Jean, Thavonekham, Bounkham, Fazal, Gulrez, Goulet, Sylvie, Jakalian, Araz, Wernic, Dominic, Tsantrizos, Youla, Poupart, Marc-André, Bös, Michael, McKercher, Ginette, Thauvette, Louise, Kukolj, George, Beaulieu, Pierre L.
Published in Bioorganic & medicinal chemistry letters (01.05.2013)
Published in Bioorganic & medicinal chemistry letters (01.05.2013)
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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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Journal Article
Indole 5-carboxamide Thumb Pocket I inhibitors of HCV NS5B polymerase with nanomolar potency in cell-based subgenomic replicons (part 2): Central amino acid linker and right-hand-side SAR studies
Beaulieu, Pierre L., Chabot, Catherine, Duan, Jianmin, Garneau, Michel, Gillard, James, Jolicoeur, Eric, Poirier, Martin, Poupart, Marc-André, Stammers, Timothy A., Kukolj, George, Tsantrizos, Youla S.
Published in Bioorganic & medicinal chemistry letters (15.06.2011)
Published in Bioorganic & medicinal chemistry letters (15.06.2011)
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Journal Article
Allosteric N-acetamide-indole-6-carboxylic acid thumb pocket 1 inhibitors of hepatitis C virus NS5B polymerase — Acylsulfonamides and acylsulfamides as carboxylic acid replacements
Beaulieu, Pierre L., Coulombe, Rene, Gillard, James, Brochu, Christian, Duan, Jianmin, Garneau, Michel, Jolicoeur, Eric, Kuhn, Peter, Poupart, Marc-Andre, Rancourt, Jean, Stammers, Timothy A., Thavonekham, Bounkham, Kukolj, George
Published in Canadian journal of chemistry (01.01.2013)
Published in Canadian journal of chemistry (01.01.2013)
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Journal Article
Immunotherapy for the First-Line Treatment of Patients with Metastatic Non-Small Cell Lung Cancer
Martinez, Pablo, Peters, Solange, Stammers, Timothy, Soria, Jean-Charles
Published in Clinical cancer research (01.05.2019)
Published in Clinical cancer research (01.05.2019)
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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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Journal Article
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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Journal Article
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
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
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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Journal Article
N-Acetamideindolecarboxylic acid allosteric ‘finger-loop’ inhibitors of the hepatitis C virus NS5B polymerase: discovery and initial optimization studies
Beaulieu, Pierre L., Jolicoeur, Eric, Gillard, James, Brochu, Christian, Coulombe, René, Dansereau, Nathalie, Duan, Jianmin, Garneau, Michel, Jakalian, Araz, Kühn, Peter, Lagacé, Lisette, LaPlante, Steven, McKercher, Ginette, Perrault, Stéphane, Poirier, Martin, Poupart, Marc-André, Stammers, Timothy, Thauvette, Louise, Thavonekham, Bounkham, Kukolj, George
Published in Bioorganic & medicinal chemistry letters (01.02.2010)
Published in Bioorganic & medicinal chemistry letters (01.02.2010)
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