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Page 1
Discovery of a novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors.
Stammers TA, Coulombe R, Rancourt J, Thavonekham B, Fazal G, Goulet S, Jakalian A, Wernic D, Tsantrizos Y, Poupart MA, Bös M, McKercher G, Thauvette L, Kukolj G, Beaulieu PL. Stammers TA, et al. Bioorg Med Chem Lett. 2013 May 1;23(9):2585-9. doi: 10.1016/j.bmcl.2013.02.110. Epub 2013 Mar 7. Bioorg Med Chem Lett. 2013. PMID: 23545108
Binding mode determination of benzimidazole inhibitors of the hepatitis C virus RNA polymerase by a structure and dynamics strategy.
LaPlante SR, Jakalian A, Aubry N, Bousquet Y, Ferland JM, Gillard J, Lefebvre S, Poirier M, Tsantrizos YS, Kukolj G, Beaulieu PL. LaPlante SR, et al. Among authors: tsantrizos ys. Angew Chem Int Ed Engl. 2004 Aug 20;43(33):4306-11. doi: 10.1002/anie.200460326. Angew Chem Int Ed Engl. 2004. PMID: 15368379 No abstract available.
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 PL, Chabot C, Duan J, Garneau M, Gillard J, Jolicoeur E, Poirier M, Poupart MA, Stammers TA, Kukolj G, Tsantrizos YS. Beaulieu PL, et al. Among authors: tsantrizos ys. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3664-70. doi: 10.1016/j.bmcl.2011.04.082. Epub 2011 Apr 24. Bioorg Med Chem Lett. 2011. PMID: 21592789
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 PL, Bös M, Cordingley MG, Chabot C, Fazal G, Garneau M, Gillard JR, Jolicoeur E, LaPlante S, McKercher G, Poirier M, Poupart MA, Tsantrizos YS, Duan J, Kukolj G. Beaulieu PL, et al. Among authors: tsantrizos ys. J Med Chem. 2012 Sep 13;55(17):7650-66. doi: 10.1021/jm3006788. Epub 2012 Aug 16. J Med Chem. 2012. PMID: 22849725
Conformation-based restrictions and scaffold replacements in the design of hepatitis C virus polymerase inhibitors: discovery of deleobuvir (BI 207127).
LaPlante SR, Bös M, Brochu C, Chabot C, Coulombe R, Gillard JR, Jakalian A, Poirier M, Rancourt J, Stammers T, Thavonekham B, Beaulieu PL, Kukolj G, Tsantrizos YS. LaPlante SR, et al. Among authors: tsantrizos ys. J Med Chem. 2014 Mar 13;57(5):1845-54. doi: 10.1021/jm4011862. Epub 2013 Nov 11. J Med Chem. 2014. PMID: 24159919
An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus.
Lamarre D, Anderson PC, Bailey M, Beaulieu P, Bolger G, Bonneau P, Bös M, Cameron DR, Cartier M, Cordingley MG, Faucher AM, Goudreau N, Kawai SH, Kukolj G, Lagacé L, LaPlante SR, Narjes H, Poupart MA, Rancourt J, Sentjens RE, St George R, Simoneau B, Steinmann G, Thibeault D, Tsantrizos YS, Weldon SM, Yong CL, Llinàs-Brunet M. Lamarre D, et al. Among authors: tsantrizos ys. Nature. 2003 Nov 13;426(6963):186-9. doi: 10.1038/nature02099. Epub 2003 Oct 26. Nature. 2003. PMID: 14578911 Free article. Clinical Trial.
Structure-activity study on a novel series of macrocyclic inhibitors of the hepatitis C virus NS3 protease leading to the discovery of BILN 2061.
Llinàs-Brunet M, Bailey MD, Bolger G, Brochu C, Faucher AM, Ferland JM, Garneau M, Ghiro E, Gorys V, Grand-Maître C, Halmos T, Lapeyre-Paquette N, Liard F, Poirier M, Rhéaume M, Tsantrizos YS, Lamarre D. Llinàs-Brunet M, et al. Among authors: tsantrizos ys. J Med Chem. 2004 Mar 25;47(7):1605-8. doi: 10.1021/jm0342414. J Med Chem. 2004. PMID: 15027850
57 results