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Page 1
Discovery of Potent, Orally Bioavailable Inhibitors of Human Cytomegalovirus.
Fader L, Brault M, Desjardins J, Dansereau N, Lamorte L, Tremblay S, Bilodeau F, Bordeleau J, Duplessis M, Gorys V, Gillard J, Gleason JL, James C, Joly MA, Kuhn C, Llinas-Brunet M, Luo L, Morency L, Morin S, Parisien M, Poirier M, Thibeault C, Trinh T, Sturino C, Srivastava S, Yoakim C, Franti M. Fader L, et al. ACS Med Chem Lett. 2016 Mar 1;7(5):525-30. doi: 10.1021/acsmedchemlett.6b00064. eCollection 2016 May 12. ACS Med Chem Lett. 2016. PMID: 27190604 Free PMC article.
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. 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: fader l. 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.
Optimization of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of HIV capsid assembly inhibitors 1: addressing configurational instability through scaffold modification.
Fader LD, Landry S, Morin S, Kawai SH, Bousquet Y, Hucke O, Goudreau N, Lemke CT, Bonneau P, Titolo S, Mason S, Simoneau B. Fader LD, et al. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3396-400. doi: 10.1016/j.bmcl.2013.03.073. Epub 2013 Mar 28. Bioorg Med Chem Lett. 2013. PMID: 23583513
Optimization of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of HIV capsid assembly inhibitors 2: structure-activity relationships (SAR) of the C3-phenyl moiety.
Fader LD, Landry S, Goulet S, Morin S, Kawai SH, Bousquet Y, Dion I, Hucke O, Goudreau N, Lemke CT, Rancourt J, Bonneau P, Titolo S, Amad M, Garneau M, Duan J, Mason S, Simoneau B. Fader LD, et al. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3401-5. doi: 10.1016/j.bmcl.2013.03.074. Epub 2013 Apr 3. Bioorg Med Chem Lett. 2013. PMID: 23601710
Preclinical profile of BI 224436, a novel HIV-1 non-catalytic-site integrase inhibitor.
Fenwick C, Amad M, Bailey MD, Bethell R, Bös M, Bonneau P, Cordingley M, Coulombe R, Duan J, Edwards P, Fader LD, Faucher AM, Garneau M, Jakalian A, Kawai S, Lamorte L, LaPlante S, Luo L, Mason S, Poupart MA, Rioux N, Schroeder P, Simoneau B, Tremblay S, Tsantrizos Y, Witvrouw M, Yoakim C. Fenwick C, et al. Among authors: fader ld. Antimicrob Agents Chemother. 2014 Jun;58(6):3233-44. doi: 10.1128/AAC.02719-13. Epub 2014 Mar 24. Antimicrob Agents Chemother. 2014. PMID: 24663024 Free PMC article.
Discovery of BI 224436, a Noncatalytic Site Integrase Inhibitor (NCINI) of HIV-1.
Fader LD, Malenfant E, Parisien M, Carson R, Bilodeau F, Landry S, Pesant M, Brochu C, Morin S, Chabot C, Halmos T, Bousquet Y, Bailey MD, Kawai SH, Coulombe R, LaPlante S, Jakalian A, Bhardwaj PK, Wernic D, Schroeder P, Amad M, Edwards P, Garneau M, Duan J, Cordingley M, Bethell R, Mason SW, Bös M, Bonneau P, Poupart MA, Faucher AM, Simoneau B, Fenwick C, Yoakim C, Tsantrizos Y. Fader LD, et al. ACS Med Chem Lett. 2014 Jan 22;5(4):422-7. doi: 10.1021/ml500002n. eCollection 2014 Apr 10. ACS Med Chem Lett. 2014. PMID: 24900852 Free PMC article.
Minimizing the Contribution of Enterohepatic Recirculation to Clearance in Rat for the NCINI Class of Inhibitors of HIV.
Fader LD, Carson R, Morin S, Bilodeau F, Chabot C, Halmos T, Bailey MD, Kawai SH, Coulombe R, Laplante S, Mekhssian K, Jakalian A, Garneau M, Duan J, Mason SW, Simoneau B, Fenwick C, Tsantrizos Y, Yoakim C. Fader LD, et al. ACS Med Chem Lett. 2014 Apr 16;5(6):711-6. doi: 10.1021/ml500110j. eCollection 2014 Jun 12. ACS Med Chem Lett. 2014. PMID: 24944749 Free PMC article.
Aligning Potency and Pharmacokinetic Properties for Pyridine-Based NCINIs.
Fader LD, Bailey M, Beaulieu E, Bilodeau F, Bonneau P, Bousquet Y, Carson RJ, Chabot C, Coulombe R, Duan J, Fenwick C, Garneau M, Halmos T, Jakalian A, James C, Kawai SH, Landry S, LaPlante SR, Mason SW, Morin S, Rioux N, Simoneau B, Surprenant S, Thavonekham B, Thibeault C, Trinh T, Tsantrizos Y, Tsoung J, Yoakim C, Wernic D. Fader LD, et al. ACS Med Chem Lett. 2016 Jun 9;7(8):797-801. doi: 10.1021/acsmedchemlett.6b00194. eCollection 2016 Aug 11. ACS Med Chem Lett. 2016. PMID: 27563405 Free PMC article.
Discovery of Potent and Orally Bioavailable Pyrimidine Amide cGAS Inhibitors via Structure-Guided Hybridization.
Cyr P, Fader LD, Burch JD, Pike KA, Sietsema DV, Boily MO, Ciblat S, Sgarioto N, Skeldon AM, Gaudreault S, Le Gros P, Dumais V, McKay DJJ, Abraham NS, Seliniotakis R, Beveridge RE. Cyr P, et al. Among authors: fader ld. ACS Med Chem Lett. 2024 Nov 25;15(12):2201-2209. doi: 10.1021/acsmedchemlett.4c00471. eCollection 2024 Dec 12. ACS Med Chem Lett. 2024. PMID: 39691514
31 results