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Discovery of GS-7682, a Novel 4'-Cyano-Modified C-Nucleoside Prodrug with Broad Activity against Pneumo- and Picornaviruses and Efficacy in RSV-Infected African Green Monkeys.
Siegel DS, Hui HC, Pitts J, Vermillion MS, Ishida K, Rautiola D, Keeney M, Irshad H, Zhang L, Chun K, Chin G, Goyal B, Doerffler E, Yang H, Clarke MO, Palmiotti C, Vijjapurapu A, Riola NC, Stray K, Murakami E, Ma B, Wang T, Zhao X, Xu Y, Lee G, Marchand B, Seung M, Nayak A, Tomkinson A, Kadrichu N, Ellis S, Barauskas O, Feng JY, Perry JK, Perron M, Bilello JP, Kuehl PJ, Subramanian R, Cihlar T, Mackman RL. Siegel DS, et al. Among authors: stray k. J Med Chem. 2024 Aug 8;67(15):12945-12968. doi: 10.1021/acs.jmedchem.4c00899. Epub 2024 Jul 17. J Med Chem. 2024. PMID: 39018526
Discovery of an oral respiratory syncytial virus (RSV) fusion inhibitor (GS-5806) and clinical proof of concept in a human RSV challenge study.
Mackman RL, Sangi M, Sperandio D, Parrish JP, Eisenberg E, Perron M, Hui H, Zhang L, Siegel D, Yang H, Saunders O, Boojamra C, Lee G, Samuel D, Babaoglu K, Carey A, Gilbert BE, Piedra PA, Strickley R, Iwata Q, Hayes J, Stray K, Kinkade A, Theodore D, Jordan R, Desai M, Cihlar T. Mackman RL, et al. Among authors: stray k. J Med Chem. 2015 Feb 26;58(4):1630-43. doi: 10.1021/jm5017768. Epub 2015 Jan 27. J Med Chem. 2015. PMID: 25574686 Clinical Trial.
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. Among authors: stray km. 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
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. Among authors: stray k. 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. Among authors: stray km. Nature. 2016 Mar 17;531(7594):381-5. doi: 10.1038/nature17180. Epub 2016 Mar 2. Nature. 2016. PMID: 26934220 Free PMC article.
Synthesis and significant cytostatic activity of 7-hetaryl-7-deazaadenosines.
Bourderioux A, Naus P, Perlíková P, Pohl R, Pichová I, Votruba I, Dzubák P, Konecný P, Hajdúch M, Stray KM, Wang T, Ray AS, Feng JY, Birkus G, Cihlar T, Hocek M. Bourderioux A, et al. J Med Chem. 2011 Aug 11;54(15):5498-507. doi: 10.1021/jm2005173. Epub 2011 Jul 11. J Med Chem. 2011. PMID: 21711054
34 results