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Items: 1 to 20 of 101

1.

Metabolic activation of the anti-hepatitis C virus nucleotide prodrug PSI-352938.

Niu C, Tolstykh T, Bao H, Park Y, Babusis D, Lam AM, Bansal S, Du J, Chang W, Reddy PG, Zhang HR, Woolley J, Wang LQ, Chao PB, Ray AS, Otto MJ, Sofia MJ, Furman PA, Murakami E.

Antimicrob Agents Chemother. 2012 Jul;56(7):3767-75. doi: 10.1128/AAC.00530-12. Epub 2012 Apr 23.

2.

Inhibition of hepatitis C virus replicon RNA synthesis by PSI-352938, a cyclic phosphate prodrug of β-D-2'-deoxy-2'-α-fluoro-2'-β-C-methylguanosine.

Lam AM, Espiritu C, Murakami E, Zennou V, Bansal S, Micolochick Steuer HM, Niu C, Keilman M, Bao H, Bourne N, Veselenak RL, Reddy PG, Chang W, Du J, Nagarathnam D, Sofia MJ, Otto MJ, Furman PA.

Antimicrob Agents Chemother. 2011 Jun;55(6):2566-75. doi: 10.1128/AAC.00032-11. Epub 2011 Mar 28.

3.

Activity and the metabolic activation pathway of the potent and selective hepatitis C virus pronucleotide inhibitor PSI-353661.

Furman PA, Murakami E, Niu C, Lam AM, Espiritu C, Bansal S, Bao H, Tolstykh T, Micolochick Steuer H, Keilman M, Zennou V, Bourne N, Veselenak RL, Chang W, Ross BS, Du J, Otto MJ, Sofia MJ.

Antiviral Res. 2011 Aug;91(2):120-32. doi: 10.1016/j.antiviral.2011.05.003. Epub 2011 May 12.

4.

Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977.

Murakami E, Tolstykh T, Bao H, Niu C, Steuer HM, Bao D, Chang W, Espiritu C, Bansal S, Lam AM, Otto MJ, Sofia MJ, Furman PA.

J Biol Chem. 2010 Nov 5;285(45):34337-47. doi: 10.1074/jbc.M110.161802. Epub 2010 Aug 26.

5.

Hepatitis C virus nucleotide inhibitors PSI-352938 and PSI-353661 exhibit a novel mechanism of resistance requiring multiple mutations within replicon RNA.

Lam AM, Espiritu C, Bansal S, Micolochick Steuer HM, Zennou V, Otto MJ, Furman PA.

J Virol. 2011 Dec;85(23):12334-42. doi: 10.1128/JVI.05639-11. Epub 2011 Sep 28.

6.

Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species.

Ma H, Jiang WR, Robledo N, Leveque V, Ali S, Lara-Jaime T, Masjedizadeh M, Smith DB, Cammack N, Klumpp K, Symons J.

J Biol Chem. 2007 Oct 12;282(41):29812-20. Epub 2007 Aug 13.

7.

Stereoselective synthesis of PSI-352938: a β-D-2'-deoxy-2'-α-fluoro-2'-β-C-methyl-3',5'-cyclic phosphate nucleotide prodrug for the treatment of HCV.

Reddy PG, Chun BK, Zhang HR, Rachakonda S, Ross BS, Sofia MJ.

J Org Chem. 2011 May 20;76(10):3782-90. doi: 10.1021/jo200060f. Epub 2011 Apr 19.

PMID:
21469736
8.

Mechanism of activation of beta-D-2'-deoxy-2'-fluoro-2'-c-methylcytidine and inhibition of hepatitis C virus NS5B RNA polymerase.

Murakami E, Bao H, Ramesh M, McBrayer TR, Whitaker T, Micolochick Steuer HM, Schinazi RF, Stuyver LJ, Obikhod A, Otto MJ, Furman PA.

Antimicrob Agents Chemother. 2007 Feb;51(2):503-9. Epub 2006 Nov 13.

9.

The mechanism of action of beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine involves a second metabolic pathway leading to beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase.

Murakami E, Niu C, Bao H, Micolochick Steuer HM, Whitaker T, Nachman T, Sofia MA, Wang P, Otto MJ, Furman PA.

Antimicrob Agents Chemother. 2008 Feb;52(2):458-64. Epub 2007 Nov 12.

10.

PSI-7851, a pronucleotide of beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine monophosphate, is a potent and pan-genotype inhibitor of hepatitis C virus replication.

Lam AM, Murakami E, Espiritu C, Steuer HM, Niu C, Keilman M, Bao H, Zennou V, Bourne N, Julander JG, Morrey JD, Smee DF, Frick DN, Heck JA, Wang P, Nagarathnam D, Ross BS, Sofia MJ, Otto MJ, Furman PA.

Antimicrob Agents Chemother. 2010 Aug;54(8):3187-96. doi: 10.1128/AAC.00399-10. Epub 2010 Jun 1.

11.

Discovery of a β-d-2'-deoxy-2'-α-fluoro-2'-β-C-methyluridine nucleotide prodrug (PSI-7977) for the treatment of hepatitis C virus.

Sofia MJ, Bao D, Chang W, Du J, Nagarathnam D, Rachakonda S, Reddy PG, Ross BS, Wang P, Zhang HR, Bansal S, Espiritu C, Keilman M, Lam AM, Steuer HM, Niu C, Otto MJ, Furman PA.

J Med Chem. 2010 Oct 14;53(19):7202-18. doi: 10.1021/jm100863x.

PMID:
20845908
12.

2'-deoxy-2'-α-fluoro-2'-β-C-methyl 3',5'-cyclic phosphate nucleotide prodrug analogs as inhibitors of HCV NS5B polymerase: discovery of PSI-352938.

Reddy PG, Bao D, Chang W, Chun BK, Du J, Nagarathnam D, Rachakonda S, Ross BS, Zhang HR, Bansal S, Espiritu CL, Keilman M, Lam AM, Niu C, Steuer HM, Furman PA, Otto MJ, Sofia MJ.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7376-80. doi: 10.1016/j.bmcl.2010.10.035. Epub 2010 Oct 15.

PMID:
21050754
13.

β-D-2'-α-F-2'-β-C-Methyl-6-O-substituted 3',5'-cyclic phosphate nucleotide prodrugs as inhibitors of hepatitis C virus replication: a structure-activity relationship study.

Du J, Bao D, Chun BK, Jiang Y, Reddy PG, Zhang HR, Ross BS, Bansal S, Bao H, Espiritu C, Lam AM, Murakami E, Niu C, Micolochick Steuer HM, Furman PA, Otto MJ, Sofia MJ.

Bioorg Med Chem Lett. 2012 Sep 15;22(18):5924-9. doi: 10.1016/j.bmcl.2012.07.066. Epub 2012 Jul 27.

PMID:
22892115
14.

A 2'-deoxy-2'-fluoro-2'-C-methyl uridine cyclopentyl carbocyclic analog and its phosphoramidate prodrug as inhibitors of HCV NS5B polymerase.

Liu J, Du J, Wang P, Nagarathnam D, Espiritu CL, Bao H, Murakami E, Furman PA, Sofia MJ.

Nucleosides Nucleotides Nucleic Acids. 2012 Apr;31(4):277-85. doi: 10.1080/15257770.2012.658131.

PMID:
22444190
15.

Inhibition of hepatitis C virus replication by GS-6620, a potent C-nucleoside monophosphate prodrug.

Feng JY, Cheng G, Perry J, Barauskas O, Xu Y, Fenaux M, Eng S, Tirunagari N, Peng B, Yu M, Tian Y, Lee YJ, Stepan G, Lagpacan LL, Jin D, Hung M, Ku KS, Han B, Kitrinos K, Perron M, Birkus G, Wong KA, Zhong W, Kim CU, Carey A, Cho A, Ray AS.

Antimicrob Agents Chemother. 2014;58(4):1930-42. doi: 10.1128/AAC.02351-13. Epub 2014 Jan 13.

16.

Selected replicon variants with low-level in vitro resistance to the hepatitis C virus NS5B polymerase inhibitor PSI-6130 lack cross-resistance with R1479.

Ali S, Leveque V, Le Pogam S, Ma H, Philipp F, Inocencio N, Smith M, Alker A, Kang H, Najera I, Klumpp K, Symons J, Cammack N, Jiang WR.

Antimicrob Agents Chemother. 2008 Dec;52(12):4356-69. doi: 10.1128/AAC.00444-08. Epub 2008 Oct 6.

17.

Synthesis of stable isotope labeled analogs of the anti-hepatitis C virus nucleotide prodrugs PSI-7977 and PSI-352938.

Chun BK, Du J, Zhang HR, Chang W, Ross BS, Jiang Y, Bao D, Espiritu CL, Keilman M, Steuer HM, Furman PA, Sofia MJ.

Nucleosides Nucleotides Nucleic Acids. 2011 Nov;30(11):886-96. doi: 10.1080/15257770.2011.614308.

PMID:
22060553
18.

Anti-hepatitis C virus activity of novel beta-d-2'-C-methyl-4'-azido pyrimidine nucleoside phosphoramidate prodrugs.

Rondla R, Coats SJ, McBrayer TR, Grier J, Johns M, Tharnish PM, Whitaker T, Zhou L, Schinazi RF.

Antivir Chem Chemother. 2009 Oct 19;20(2):99-106. doi: 10.3851/IMP1400.

PMID:
19843980
19.

Resistance analysis and characterization of NITD008 as an adenosine analog inhibitor against hepatitis C virus.

Qing J, Luo R, Wang Y, Nong J, Wu M, Shao Y, Tang R, Yu X, Yin Z, Sun Y.

Antiviral Res. 2016 Feb;126:43-54. doi: 10.1016/j.antiviral.2015.12.010. Epub 2015 Dec 24.

PMID:
26724382
20.

Antiviral efficacy upon administration of a HepDirect prodrug of 2'-C-methylcytidine to hepatitis C virus-infected chimpanzees.

Carroll SS, Koeplinger K, Vavrek M, Zhang NR, Handt L, MacCoss M, Olsen DB, Reddy KR, Sun Z, van Poelje PD, Fujitaki JM, Boyer SH, Linemeyer DL, Hecker SJ, Erion MD.

Antimicrob Agents Chemother. 2011 Aug;55(8):3854-60. doi: 10.1128/AAC.01152-10. Epub 2011 May 31.

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