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Items: 18

1.

Coronavirus Susceptibility to the Antiviral Remdesivir (GS-5734) Is Mediated by the Viral Polymerase and the Proofreading Exoribonuclease.

Agostini ML, Andres EL, Sims AC, Graham RL, Sheahan TP, Lu X, Smith EC, Case JB, Feng JY, Jordan R, Ray AS, Cihlar T, Siegel D, Mackman RL, Clarke MO, Baric RS, Denison MR.

MBio. 2018 Mar 6;9(2). pii: e00221-18. doi: 10.1128/mBio.00221-18.

2.

Broad-spectrum antiviral GS-5734 inhibits both epidemic and zoonotic coronaviruses.

Sheahan TP, Sims AC, Graham RL, Menachery VD, Gralinski LE, Case JB, Leist SR, Pyrc K, Feng JY, Trantcheva I, Bannister R, Park Y, Babusis D, Clarke MO, Mackman RL, Spahn JE, Palmiotti CA, Siegel D, Ray AS, Cihlar T, Jordan R, Denison MR, Baric RS.

Sci Transl Med. 2017 Jun 28;9(396). pii: eaal3653. doi: 10.1126/scitranslmed.aal3653.

3.

Discovery of a 2'-fluoro-2'-C-methyl C-nucleotide HCV polymerase inhibitor and a phosphoramidate prodrug with favorable properties.

Kirschberg TA, Metobo S, Clarke MO, Aktoudianakis V, Babusis D, Barauskas O, Birkus G, Butler T, Byun D, Chin G, Doerffler E, Edwards TE, Fenaux M, Lee R, Lew W, Mish MR, Murakami E, Park Y, Squires NH, Tirunagari N, Wang T, Whitcomb M, Xu J, Yang H, Ye H, Zhang L, Appleby TC, Feng JY, Ray AS, Cho A, Kim CU.

Bioorg Med Chem Lett. 2017 Apr 15;27(8):1840-1847. doi: 10.1016/j.bmcl.2017.02.037. Epub 2017 Feb 20.

PMID:
28274633
4.

GS-5734 and its parent nucleoside analog inhibit Filo-, Pneumo-, and Paramyxoviruses.

Lo MK, Jordan R, Arvey A, Sudhamsu J, Shrivastava-Ranjan P, Hotard AL, Flint M, McMullan LK, Siegel D, Clarke MO, Mackman RL, Hui HC, Perron M, Ray AS, Cihlar T, Nichol ST, Spiropoulou CF.

Sci Rep. 2017 Mar 6;7:43395. doi: 10.1038/srep43395.

5.

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.

J Med Chem. 2017 Mar 9;60(5):1648-1661. doi: 10.1021/acs.jmedchem.6b01594. Epub 2017 Feb 14.

PMID:
28124907
6.

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.

Nature. 2016 Mar 17;531(7594):381-5. doi: 10.1038/nature17180. Epub 2016 Mar 2. Erratum in: ACS Chem Biol. 2016 May 20;11(5):1463.

7.

Discovery of β-D-2'-deoxy-2'-α-fluoro-4'-α-cyano-5-aza-7,9-dideaza adenosine as a potent nucleoside inhibitor of respiratory syncytial virus with excellent selectivity over mitochondrial RNA and DNA polymerases.

Clarke MO, Mackman R, Byun D, Hui H, Barauskas O, Birkus G, Chun BK, Doerffler E, Feng J, Karki K, Lee G, Perron M, Siegel D, Swaminathan S, Lee W.

Bioorg Med Chem Lett. 2015 Jun 15;25(12):2484-7. doi: 10.1016/j.bmcl.2015.04.073. Epub 2015 Apr 29.

PMID:
25978965
8.

A small-molecule inhibitor of hepatitis C virus infectivity.

Bush CO, Pokrovskii MV, Saito R, Morganelli P, Canales E, Clarke MO, Lazerwith SE, Golde J, Reid BG, Babaoglu K, Pagratis N, Zhong W, Delaney WE 4th, Paulson MS, Beran RK.

Antimicrob Agents Chemother. 2014;58(1):386-96. doi: 10.1128/AAC.02083-13. Epub 2013 Oct 28.

9.

Discovery of GS-9669, a thumb site II non-nucleoside inhibitor of NS5B for the treatment of genotype 1 chronic hepatitis C infection.

Lazerwith SE, Lew W, Zhang J, Morganelli P, Liu Q, Canales E, Clarke MO, Doerffler E, Byun D, Mertzman M, Ye H, Chong L, Xu L, Appleby T, Chen X, Fenaux M, Hashash A, Leavitt SA, Mabery E, Matles M, Mwangi JW, Tian Y, Lee YJ, Zhang J, Zhu C, Murray BP, Watkins WJ.

J Med Chem. 2014 Mar 13;57(5):1893-901. doi: 10.1021/jm401420j. Epub 2013 Nov 6.

PMID:
24144213
10.

Preclinical characterization of GS-9669, a thumb site II inhibitor of the hepatitis C virus NS5B polymerase.

Fenaux M, Eng S, Leavitt SA, Lee YJ, Mabery EM, Tian Y, Byun D, Canales E, Clarke MO, Doerffler E, Lazerwith SE, Lew W, Liu Q, Mertzman M, Morganelli P, Xu L, Ye H, Zhang J, Matles M, Murray BP, Mwangi J, Zhang J, Hashash A, Krawczyk SH, Bidgood AM, Appleby TC, Watkins WJ.

Antimicrob Agents Chemother. 2013 Feb;57(2):804-10. doi: 10.1128/AAC.02052-12. Epub 2012 Nov 26.

11.

Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.

Sheng XC, Appleby T, Butler T, Cai R, Chen X, Cho A, Clarke MO, Cottell J, Delaney WE 4th, Doerffler E, Link J, Ji M, Pakdaman R, Pyun HJ, Wu Q, Xu J, Kim CU.

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2629-34. doi: 10.1016/j.bmcl.2012.01.017. Epub 2012 Feb 1.

PMID:
22366653
12.

Discovery of GS-9256: a novel phosphinic acid derived inhibitor of the hepatitis C virus NS3/4A protease with potent clinical activity.

Sheng XC, Casarez A, Cai R, Clarke MO, Chen X, Cho A, Delaney WE 4th, Doerffler E, Ji M, Mertzman M, Pakdaman R, Pyun HJ, Rowe T, Wu Q, Xu J, Kim CU.

Bioorg Med Chem Lett. 2012 Feb 1;22(3):1394-6. doi: 10.1016/j.bmcl.2011.12.038. Epub 2011 Dec 13.

PMID:
22244938
13.

Novel, potent and orally bioavailable indolizidinone-derived inhibitors of the hepatitis C virus NS3 protease.

Clarke MO, Byun D, Chen X, Doerffler E, Leavitt SA, Sheng XC, Yang CY, Kim CU.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1095-8. doi: 10.1016/j.bmcl.2011.11.107. Epub 2011 Dec 6.

PMID:
22189140
14.

Optimization of Pharmacokinetics through Manipulation of Physicochemical Properties in a Series of HCV Inhibitors.

Lazerwith SE, Bahador G, Canales E, Cheng G, Chong L, Clarke MO, Doerffler E, Eisenberg EJ, Hayes J, Lu B, Liu Q, Matles M, Mertzman M, Mitchell ML, Morganelli P, Murray BP, Robinson M, Strickley RG, Tessler M, Tirunagari N, Wang J, Wang Y, Zhang JR, Zheng X, Zhong W, Watkins WJ.

ACS Med Chem Lett. 2011 Aug 8;2(10):715-9. doi: 10.1021/ml200163b. eCollection 2011 Oct 13.

15.

Novel, potent, and orally bioavailable phosphinic acid inhibitors of the hepatitis C virus NS3 protease.

Clarke MO, Chen X, Cho A, Delaney WE 4th, Doerffler E, Fardis M, Ji M, Mertzman M, Pakdaman R, Pyun HJ, Rowe T, Yang CY, Sheng XC, Kim CU.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3568-72. doi: 10.1016/j.bmcl.2011.04.125. Epub 2011 May 3.

PMID:
21601450
16.

Function oriented synthesis: the design, synthesis, PKC binding and translocation activity of a new bryostatin analog.

Wender PA, Baryza JL, Brenner SE, Clarke MO, Craske ML, Horan JC, Meyer T.

Curr Drug Discov Technol. 2004 Jan;1(1):1-11.

PMID:
16472215
17.
18.

The practical synthesis of a novel and highly potent analogue of bryostatin.

Wender PA, Baryza JL, Bennett CE, Bi FC, Brenner SE, Clarke MO, Horan JC, Kan C, Lacôte E, Lippa B, Nell PG, Turner TM.

J Am Chem Soc. 2002 Nov 20;124(46):13648-9.

PMID:
12431074

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