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Discovery of GS-5245 (Obeldesivir), an Oral Prodrug of Nucleoside GS-441524 That Exhibits Antiviral Efficacy in SARS-CoV-2-Infected African Green Monkeys.
Mackman RL, Kalla RV, Babusis D, Pitts J, Barrett KT, Chun K, Du Pont V, Rodriguez L, Moshiri J, Xu Y, Lee M, Lee G, Bleier B, Nguyen AQ, O'Keefe BM, Ambrosi A, Cook M, Yu J, Dempah KE, Bunyan E, Riola NC, Lu X, Liu R, Davie A, Hsiang TY, Dearing J, Vermillion M, Gale M Jr, Niedziela-Majka A, Feng JY, Hedskog C, Bilello JP, Subramanian R, Cihlar T. Mackman RL, et al. J Med Chem. 2023 Sep 14;66(17):11701-11717. doi: 10.1021/acs.jmedchem.3c00750. Epub 2023 Aug 19. J Med Chem. 2023. PMID: 37596939
Prodrugs of a 1'-CN-4-Aza-7,9-dideazaadenosine C-Nucleoside Leading to the Discovery of Remdesivir (GS-5734) as a Potent Inhibitor of Respiratory Syncytial Virus with Efficacy in the African Green Monkey Model of RSV.
Mackman RL, Hui HC, Perron M, Murakami E, Palmiotti C, Lee G, Stray K, Zhang L, Goyal B, Chun K, Byun D, Siegel D, Simonovich S, Du Pont V, Pitts J, Babusis D, Vijjapurapu A, Lu X, Kim C, Zhao X, Chan J, Ma B, Lye D, Vandersteen A, Wortman S, Barrett KT, Toteva M, Jordan R, Subramanian R, Bilello JP, Cihlar T. Mackman RL, et al. J Med Chem. 2021 Apr 22;64(8):5001-5017. doi: 10.1021/acs.jmedchem.1c00071. Epub 2021 Apr 9. J Med Chem. 2021. PMID: 33835812
Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys.
Warren TK, Jordan R, Lo MK, Ray AS, Mackman RL, Soloveva V, Siegel D, Perron M, Bannister R, Hui HC, Larson N, Strickley R, Wells J, Stuthman KS, Van Tongeren SA, Garza NL, Donnelly G, Shurtleff AC, Retterer CJ, Gharaibeh D, Zamani R, Kenny T, Eaton BP, Grimes E, Welch LS, Gomba L, Wilhelmsen CL, Nichols DK, Nuss JE, Nagle ER, Kugelman JR, Palacios G, Doerffler E, Neville S, Carra E, Clarke MO, Zhang L, Lew W, Ross B, Wang Q, Chun K, Wolfe L, Babusis D, Park Y, Stray KM, Trancheva I, Feng JY, Barauskas O, Xu Y, Wong P, Braun MR, Flint M, McMullan LK, Chen SS, Fearns R, Swaminathan S, Mayers DL, Spiropoulou CF, Lee WA, Nichol ST, Cihlar T, Bavari S. Warren TK, et al. Nature. 2016 Mar 17;531(7594):381-5. doi: 10.1038/nature17180. Epub 2016 Mar 2. Nature. 2016. PMID: 26934220 Free PMC article.
Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses.
Siegel D, Hui HC, Doerffler E, Clarke MO, Chun K, Zhang L, Neville S, Carra E, Lew W, Ross B, Wang Q, Wolfe L, Jordan R, Soloveva V, Knox J, Perry J, Perron M, Stray KM, Barauskas O, Feng JY, Xu Y, Lee G, Rheingold AL, Ray AS, Bannister R, Strickley R, Swaminathan S, Lee WA, Bavari S, Cihlar T, Lo MK, Warren TK, Mackman RL. Siegel D, et al. J Med Chem. 2017 Mar 9;60(5):1648-1661. doi: 10.1021/acs.jmedchem.6b01594. Epub 2017 Feb 14. J Med Chem. 2017. PMID: 28124907