Beaulieu PL - Search Results

1

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: beaulieu pl. J Med Chem. 2014 Mar 13;57(5):1932-43. doi: 10.1021/jm4004522. Epub 2013 Jul 12. J Med Chem. 2014. PMID: 23773186

2

Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: discovery and preliminary SAR of benzimidazole derivatives.

Beaulieu PL, Bös M, Bousquet Y, Fazal G, Gauthier J, Gillard J, Goulet S, LaPlante S, Poupart MA, Lefebvre S, McKercher G, Pellerin C, Austel V, Kukolj G. Beaulieu PL, et al. Bioorg Med Chem Lett. 2004 Jan 5;14(1):119-24. doi: 10.1016/j.bmcl.2003.10.023. Bioorg Med Chem Lett. 2004. PMID: 14684311

3

Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: discovery of benzimidazole 5-carboxylic amide derivatives with low-nanomolar potency.

Beaulieu PL, Bös M, Bousquet Y, DeRoy P, Fazal G, Gauthier J, Gillard J, Goulet S, McKercher G, Poupart MA, Valois S, Kukolj G. Beaulieu PL, et al. Bioorg Med Chem Lett. 2004 Feb 23;14(4):967-71. doi: 10.1016/j.bmcl.2003.12.032. Bioorg Med Chem Lett. 2004. PMID: 15013003

4

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 PL, Bousquet Y, Gauthier J, Gillard J, Marquis M, McKercher G, Pellerin C, Valois S, Kukolj G. Beaulieu PL, et al. J Med Chem. 2004 Dec 30;47(27):6884-92. doi: 10.1021/jm040134d. J Med Chem. 2004. PMID: 15615537

5

Binding site characterization and resistance to a class of non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase.

Kukolj G, McGibbon GA, McKercher G, Marquis M, Lefèbvre S, Thauvette L, Gauthier J, Goulet S, Poupart MA, Beaulieu PL. Kukolj G, et al. Among authors: beaulieu pl. J Biol Chem. 2005 Nov 25;280(47):39260-7. doi: 10.1074/jbc.M506407200. Epub 2005 Sep 27. J Biol Chem. 2005. PMID: 16188890 Free article.

6

Improved replicon cellular activity of non-nucleoside allosteric inhibitors of HCV NS5B polymerase: from benzimidazole to indole scaffolds.

Beaulieu PL, Gillard J, Bykowski D, Brochu C, Dansereau N, Duceppe JS, Haché B, Jakalian A, Lagacé L, LaPlante S, McKercher G, Moreau E, Perreault S, Stammers T, Thauvette L, Warrington J, Kukolj G. Beaulieu PL, et al. Bioorg Med Chem Lett. 2006 Oct 1;16(19):4987-93. doi: 10.1016/j.bmcl.2006.07.074. Bioorg Med Chem Lett. 2006. PMID: 16908138

7

Discovery of benzimidazole-diamide finger loop (Thumb Pocket I) allosteric inhibitors of HCV NS5B polymerase: Implementing parallel synthesis for rapid linker optimization.

Goulet S, Poupart MA, Gillard J, Poirier M, Kukolj G, Beaulieu PL. Goulet S, et al. Among authors: beaulieu pl. Bioorg Med Chem Lett. 2010 Jan 1;20(1):196-200. doi: 10.1016/j.bmcl.2009.10.136. Epub 2009 Nov 4. Bioorg Med Chem Lett. 2010. PMID: 19945870

8

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. 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

9

Benzimidazole Thumb Pocket I finger-loop inhibitors of HCV NS5B polymerase: improved drug-like properties through C-2 SAR in three sub-series.

Beaulieu PL, Dansereau N, Duan J, Garneau M, Gillard J, McKercher G, LaPlante S, Lagacée L, Thauvette L, Kukolj G. Beaulieu PL, et al. Bioorg Med Chem Lett. 2010 Mar 15;20(6):1825-9. doi: 10.1016/j.bmcl.2010.02.003. Epub 2010 Feb 6. Bioorg Med Chem Lett. 2010. PMID: 20185309

10

Importance of ligand bioactive conformation in the discovery of potent indole-diamide inhibitors of the hepatitis C virus NS5B.

LaPlante SR, Gillard JR, Jakalian A, Aubry N, Coulombe R, Brochu C, Tsantrizos YS, Poirier M, Kukolj G, Beaulieu PL. LaPlante SR, et al. Among authors: beaulieu pl. J Am Chem Soc. 2010 Nov 3;132(43):15204-12. doi: 10.1021/ja101358s. J Am Chem Soc. 2010. PMID: 20942454

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