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Page 1
Anthranilic acid-based Thumb Pocket 2 HCV NS5B polymerase inhibitors with sub-micromolar potency in the cell-based replicon assay.
Stammers TA, Coulombe R, Duplessis M, Fazal G, Gagnon A, Garneau M, Goulet S, Jakalian A, LaPlante S, Rancourt J, Thavonekham B, Wernic D, Kukolj G, Beaulieu PL. Stammers TA, et al. Among authors: coulombe r. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6879-85. doi: 10.1016/j.bmcl.2013.09.102. Epub 2013 Oct 8. Bioorg Med Chem Lett. 2013. PMID: 24176401
Thiotetrazole alkynylacetanilides as potent and bioavailable non-nucleoside inhibitors of the HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases.
Gagnon A, Amad MH, Bonneau PR, Coulombe R, DeRoy PL, Doyon L, Duan J, Garneau M, Guse I, Jakalian A, Jolicoeur E, Landry S, Malenfant E, Simoneau B, Yoakim C. Gagnon A, et al. Among authors: coulombe r. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4437-41. doi: 10.1016/j.bmcl.2007.06.012. Epub 2007 Jun 8. Bioorg Med Chem Lett. 2007. PMID: 17583503
N-Acetamideindolecarboxylic acid allosteric 'finger-loop' inhibitors of the hepatitis C virus NS5B polymerase: discovery and initial optimization studies.
Beaulieu PL, Jolicoeur E, Gillard J, Brochu C, Coulombe R, Dansereau N, Duan J, Garneau M, Jakalian A, Kühn P, Lagacé L, LaPlante S, McKercher G, Perrault S, Poirier M, Poupart MA, Stammers T, Thauvette L, Thavonekham B, Kukolj G. Beaulieu PL, et al. Among authors: coulombe r. Bioorg Med Chem Lett. 2010 Feb 1;20(3):857-61. doi: 10.1016/j.bmcl.2009.12.101. Epub 2010 Jan 4. Bioorg Med Chem Lett. 2010. PMID: 20074949
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. Among authors: coulombe r. 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
Structure-based design of novel HCV NS5B thumb pocket 2 allosteric inhibitors with submicromolar gt1 replicon potency: discovery of a quinazolinone chemotype.
Beaulieu PL, Coulombe R, Duan J, Fazal G, Godbout C, Hucke O, Jakalian A, Joly MA, Lepage O, Llinàs-Brunet M, Naud J, Poirier M, Rioux N, Thavonekham B, Kukolj G, Stammers TA. Beaulieu PL, et al. Among authors: coulombe r. Bioorg Med Chem Lett. 2013 Jul 15;23(14):4132-40. doi: 10.1016/j.bmcl.2013.05.037. Epub 2013 May 23. Bioorg Med Chem Lett. 2013. PMID: 23768906
Molecular dynamics simulations and structure-based rational design lead to allosteric HCV NS5B polymerase thumb pocket 2 inhibitor with picomolar cellular replicon potency.
Hucke O, Coulombe R, Bonneau P, Bertrand-Laperle M, Brochu C, Gillard J, Joly MA, Landry S, Lepage O, Llinàs-Brunet M, Pesant M, Poirier M, Poirier M, McKercher G, Marquis M, Kukolj G, Beaulieu PL, Stammers TA. Hucke O, et al. Among authors: coulombe r. J Med Chem. 2014 Mar 13;57(5):1932-43. doi: 10.1021/jm4004522. Epub 2013 Jul 12. J Med Chem. 2014. PMID: 23773186
145 results