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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: gagnon a. 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
Inhibition of HIV-1 capsid assembly: optimization of the antiviral potency by site selective modifications at N1, C2 and C16 of a 5-(5-furan-2-yl-pyrazol-1-yl)-1H-benzimidazole scaffold.
Tremblay M, Bonneau P, Bousquet Y, DeRoy P, Duan J, Duplessis M, Gagnon A, Garneau M, Goudreau N, Guse I, Hucke O, Kawai SH, Lemke CT, Mason SW, Simoneau B, Surprenant S, Titolo S, Yoakim C. Tremblay M, et al. Among authors: gagnon a. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7512-7. doi: 10.1016/j.bmcl.2012.10.034. Epub 2012 Oct 16. Bioorg Med Chem Lett. 2012. PMID: 23122820
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 PL, Bolger G, Deon D, Duplessis M, Fazal G, Gagnon A, Garneau M, LaPlante S, Stammers T, Kukolj G, Duan J. Beaulieu PL, et al. Among authors: gagnon a. Bioorg Med Chem Lett. 2015 Mar 1;25(5):1140-5. doi: 10.1016/j.bmcl.2014.12.078. Epub 2015 Jan 3. Bioorg Med Chem Lett. 2015. PMID: 25599836
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. 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
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
Gehling VS, Vaswani RG, Nasveschuk CG, Duplessis M, Iyer P, Balasubramanian S, Zhao F, Good AC, Campbell R, Lee C, Dakin LA, Cook AS, Gagnon A, Harmange JC, Audia JE, Cummings RT, Normant E, Trojer P, Albrecht BK. Gehling VS, et al. Among authors: gagnon a. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3644-9. doi: 10.1016/j.bmcl.2015.06.056. Epub 2015 Jun 19. Bioorg Med Chem Lett. 2015. PMID: 26189078
Discovery of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of inhibitors of HIV-1 capsid assembly.
Fader LD, Bethell R, Bonneau P, Bös M, Bousquet Y, Cordingley MG, Coulombe R, Deroy P, Faucher AM, Gagnon A, Goudreau N, Grand-Maître C, Guse I, Hucke O, Kawai SH, Lacoste JE, Landry S, Lemke CT, Malenfant E, Mason S, Morin S, O'Meara J, Simoneau B, Titolo S, Yoakim C. Fader LD, et al. Among authors: gagnon a. Bioorg Med Chem Lett. 2011 Jan 1;21(1):398-404. doi: 10.1016/j.bmcl.2010.10.131. Epub 2010 Oct 31. Bioorg Med Chem Lett. 2011. PMID: 21087861
Distinct effects of two HIV-1 capsid assembly inhibitor families that bind the same site within the N-terminal domain of the viral CA protein.
Lemke CT, Titolo S, von Schwedler U, Goudreau N, Mercier JF, Wardrop E, Faucher AM, Coulombe R, Banik SS, Fader L, Gagnon A, Kawai SH, Rancourt J, Tremblay M, Yoakim C, Simoneau B, Archambault J, Sundquist WI, Mason SW. Lemke CT, et al. Among authors: gagnon a. J Virol. 2012 Jun;86(12):6643-55. doi: 10.1128/JVI.00493-12. Epub 2012 Apr 11. J Virol. 2012. PMID: 22496222 Free PMC article.
529 results