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Page 1
Concise and Practical Asymmetric Synthesis of a Challenging Atropisomeric HIV Integrase Inhibitor.
Fandrick KR, Li W, Zhang Y, Tang W, Gao J, Rodriguez S, Patel ND, Reeves DC, Wu JP, Sanyal S, Gonnella N, Qu B, Haddad N, Lorenz JC, Sidhu K, Wang J, Ma S, Grinberg N, Lee H, Tsantrizos Y, Poupart MA, Busacca CA, Yee NK, Lu BZ, Senanayake CH. Fandrick KR, et al. Among authors: tsantrizos y. Angew Chem Int Ed Engl. 2015 Jun 8;54(24):7144-8. doi: 10.1002/anie.201501575. Epub 2015 May 4. Angew Chem Int Ed Engl. 2015. PMID: 25939331
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. Nature. 2003 Nov 13;426(6963):186-9. doi: 10.1038/nature02099. Epub 2003 Oct 26. Nature. 2003. PMID: 14578911 Free article. Clinical Trial.
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. 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. J Med Chem. 2012 Sep 13;55(17):7650-66. doi: 10.1021/jm3006788. Epub 2012 Aug 16. J Med Chem. 2012. PMID: 22849725
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: tsantrizos y. 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
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: tsantrizos y. 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. Among authors: tsantrizos y. 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.
A highly concise and convergent synthesis of HCV polymerase inhibitor Deleobuvir (BI 207127): application of a one-pot borylation-Suzuki coupling reaction.
Zhang Y, Lu BZ, Li G, Rodriguez S, Tan J, Wei HX, Liu J, Roschangar F, Ding F, Zhao W, Qu B, Reeves D, Grinberg N, Lee H, Heckmann G, Niemeier O, Brenner M, Tsantrizos Y, Beaulieu PL, Hossain A, Yee N, Farina V, Senanayake CH. Zhang Y, et al. Among authors: tsantrizos y. Org Lett. 2014 Sep 5;16(17):4558-61. doi: 10.1021/ol5021114. Epub 2014 Aug 8. Org Lett. 2014. PMID: 25105303
57 results