-
1
-
-
59149085501
-
The global burden of hepatitis C
-
Lavanchy, D. The global burden of hepatitis C Liver Int. 2009, 29 (S1) 74-81
-
(2009)
Liver Int.
, vol.29
, Issue.S1
, pp. 74-81
-
-
Lavanchy, D.1
-
2
-
-
59149097207
-
Expert opinion on the treatment of patients with chronic hepatitis C
-
Zeuzem, S.; Berg, T.; Moeller, B.; Hinrichsen, H.; Mauss, S.; Wedemeyer, H.; Sarrazin, C.; Hueppe, D.; Zehnter, E.; Manns, M. P. Expert opinion on the treatment of patients with chronic hepatitis C J. Viral Hepatitis 2009, 16, 75-90
-
(2009)
J. Viral Hepatitis
, vol.16
, pp. 75-90
-
-
Zeuzem, S.1
Berg, T.2
Moeller, B.3
Hinrichsen, H.4
Mauss, S.5
Wedemeyer, H.6
Sarrazin, C.7
Hueppe, D.8
Zehnter, E.9
Manns, M.P.10
-
3
-
-
65649147492
-
A review of current anti-HCV treatment regimens and possible future strategies
-
Neukam, K.; Macias, J.; Mira, J. A.; Pineda, J. A. A review of current anti-HCV treatment regimens and possible future strategies Expert Opin. Pharmacother. 2009, 10, 417-433
-
(2009)
Expert Opin. Pharmacother.
, vol.10
, pp. 417-433
-
-
Neukam, K.1
MacIas, J.2
Mira, J.A.3
Pineda, J.A.4
-
4
-
-
74049117015
-
HCV drug discovery aimed at viral eradication
-
Schinazi, R. F.; Bassit, L.; Gavegnano, C. HCV drug discovery aimed at viral eradication J. Viral Hepatitis 2010, 17, 77-90
-
(2010)
J. Viral Hepatitis
, vol.17
, pp. 77-90
-
-
Schinazi, R.F.1
Bassit, L.2
Gavegnano, C.3
-
5
-
-
77953463393
-
Nucleoside analogue inhibitors of hepatitis C viral replication: Recent advances, challenges and trends
-
Furman, P. A.; Lam, A. M.; Murakami, E. Nucleoside analogue inhibitors of hepatitis C viral replication: recent advances, challenges and trends Future Med. Chem. 2009, 1, 1429-1452
-
(2009)
Future Med. Chem.
, vol.1
, pp. 1429-1452
-
-
Furman, P.A.1
Lam, A.M.2
Murakami, E.3
-
6
-
-
78649495797
-
Nucleoside analogue inhibitors of hepatitis C viral replication
-
Ed.; American Society for Microbiology: Washington, DC
-
Carroll, S. S.; La Femina, R. L. Nucleoside analogue inhibitors of hepatitis C viral replication. In Antiviral Research; La Femina, R. L., Ed.; American Society for Microbiology: Washington, DC, 2009; pp 153 - 166.
-
(2009)
Antiviral Research
, pp. 153-166
-
-
Carroll, S.S.1
La Femina, R.L.2
La Femina, R.L.3
-
7
-
-
33646457538
-
Inhibition of hepatitis C replicon RNA synthesis by β- D -2′-deoxy-2′-fluoro-2′-C-methylcytidine: A specific inhibitor of hepatitis C virus replication
-
Stuyver, L. J.; McBrayer, T. R.; Tharnish, P. M.; Clark, J. L.; Hollecher, L.; Lostia, S.; Nachman, T.; Grier, J.; Bennett, M. A.; Xie, M.-Y.; Schinazi, R. F.; Morrey, J. D.; Julander, J. L.; Furman, P. A.; Otto, M. J. Inhibition of hepatitis C replicon RNA synthesis by β- d -2′-deoxy-2′-fluoro-2′-C-methylcytidine: a specific inhibitor of hepatitis C virus replication Antiviral Chem. Chemother. 2006, 17, 79-87
-
(2006)
Antiviral Chem. Chemother.
, vol.17
, pp. 79-87
-
-
Stuyver, L.J.1
McBrayer, T.R.2
Tharnish, P.M.3
Clark, J.L.4
Hollecher, L.5
Lostia, S.6
Nachman, T.7
Grier, J.8
Bennett, M.A.9
Xie, M.-Y.10
Schinazi, R.F.11
Morrey, J.D.12
Julander, J.L.13
Furman, P.A.14
Otto, M.J.15
-
8
-
-
38649112300
-
The mechanism of action of β-D-2′-deoxy-2′-fluoro- 2′-C-methylcytidine involves a second metabolic pathway leading to β-D-2′-deoxy-2′-fluoro-2′-C-methyluridine 5′-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase
-
DOI 10.1128/AAC.01184-07
-
Murakami, E.; Niu, C.; Bao, H.; Steuer, H. M.; Whitaker, T.; Nachman, T.; Sofia, M. A.; Wang, P.; Otto, M. J.; Furman, P. A. The mechanism of action of β- d -2′-deoxy-2′-fluoro-2′- C -methylcytidine involves a second metabolic pathway leading to β- d -2′-deoxy-2′-fluoro- 2′- C -methyluridine 5′-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase Antimicrob. Agents Chemother. 2008, 52, 458-464 (Pubitemid 351170814)
-
(2008)
Antimicrobial Agents and Chemotherapy
, vol.52
, Issue.2
, pp. 458-464
-
-
Murakami, E.1
Niu, C.2
Bao, H.3
Micolochick Steuer, H.M.4
Whitaker, T.5
Nachman, T.6
Sofia, M.A.7
Wang, P.8
Otto, M.J.9
Furman, P.A.10
-
9
-
-
77953415345
-
No evidence of R7128 drug resistance after up to 4 weeks treatment of GT 1, 2 and 3 hepatitis C virus infected individuals
-
Copenhagen, Denmark, April,; Abstr. No. 839
-
Le Pogam, S.; Kang, H.; Seshaadri, A.; Kosaka, A.; Hu, S.; Ewing, A.; Yan, J.-M.; Beard, A.; Symons, J.; Cammack, N.; Ńjera, I. No evidence of R7128 drug resistance after up to 4 weeks treatment of GT 1, 2 and 3 hepatitis C virus infected individuals. 44th Annual Meeting of the European Association for the Study of the Liver; Copenhagen, Denmark, April, 2009; Abstr. No. 839.
-
(2009)
44th Annual Meeting of the European Association for the Study of the Liver
-
-
Le Pogam, S.1
Kang, H.2
Seshaadri, A.3
Kosaka, A.4
Hu, S.5
Ewing, A.6
Yan, J.-M.7
Beard, A.8
Symons, J.9
Cammack, N.10
Ńjera, I.11
-
10
-
-
23944469297
-
Design, synthesis, and antiviral activity of 2′-deoxy-2′- fluoro-2′-C-methylcytidine, a potent inhibitor of hepatitis C virus replication
-
DOI 10.1021/jm0502788
-
Clark, J. L.; Hollecker, L.; Mason, J. C.; Stuyver, L. J.; Tharnish, P. M.; Lostia, S.; McBrayer, T. R.; Schinazi, R. F.; Watanabe, K. A.; Otto, M. J.; Furman, P. A.; Stec, W. J.; Patterson, S. E.; Pankiewicz, K. W. Design, synthesis, and antiviral activity of 2′-deoxy-2′-fluoro-2′-C- methyl-cytidine, a potent inhibitor of hepatitis C virus replication J. Med. Chem. 2005, 48, 5504-5508 (Pubitemid 41209247)
-
(2005)
Journal of Medicinal Chemistry
, vol.48
, Issue.17
, pp. 5504-5508
-
-
Clark, J.L.1
Hollecker, L.2
Mason, J.C.3
Stuyver, L.J.4
Tharnish, P.M.5
Lostia, S.6
McBrayer, T.R.7
Schinazi, R.F.8
Watanabe, K.A.9
Otto, M.J.10
Furman, P.A.11
Stec, W.J.12
Patterson, S.E.13
Pankiewicz, K.W.14
-
11
-
-
32044474268
-
Synthesis and antiviral activity of 2′-deoxy-2′-fluoro- 2′-C-methyl purine nucleosides as inhibitors of hepatitis C virus RNA replication
-
DOI 10.1016/j.bmcl.2005.12.002, PII S0960894X05015374
-
Clark, J. L.; Mason, J. C.; Hollecker, L.; Stuyver, L. J.; Tharnish, P. M.; McBrayer, T. R.; Otto, M. J.; Furman, P. A.; Schinazi, R. F.; Watanabe, K. A. Synthesis and antiviral activity of 2′-deoxy-2′-fluoro-2′- C -methyl purine nucleosides as inhibitors of hepatitis C virus RNA replication Bioorg. Med. Chem. Lett. 2006, 16, 1712-1715 (Pubitemid 43197551)
-
(2006)
Bioorganic and Medicinal Chemistry Letters
, vol.16
, Issue.6
, pp. 1712-1715
-
-
Clark, J.L.1
Mason, J.C.2
Hollecker, L.3
Stuyver, L.J.4
Tharnish, P.M.5
McBrayer, T.R.6
Otto, M.J.7
Furman, P.A.8
Schinazi, R.F.9
Watanabe, K.A.10
-
12
-
-
79951540407
-
D -2′-Deoxy-2′-fluoro-2′- C -methyl-ribofuranosyl nucleosides: Effect of base modifications on antihepatitis C virus activity
-
Washington, DC, August,; MEDI 100
-
Wang, P.; Sofia, M. J.; Chun, B.-K.; Du, J.; Rachakonda, S.; Steuer, H. M.; Murakami, E.; Bao, H.; Nagarathnam, D.; Otto, M. J.; Furman, P. A. d -2′-Deoxy-2′-fluoro-2′- C -methyl-ribofuranosyl nucleosides: Effect of base modifications on antihepatitis C virus activity. 238th ACS National Meeting, Washington, DC, August, 2009; MEDI 100.
-
(2009)
238th ACS National Meeting
-
-
Wang, P.1
Sofia, M.J.2
Chun, B.-K.3
Du, J.4
Rachakonda, S.5
Steuer, H.M.6
Murakami, E.7
Bao, H.8
Nagarathnam, D.9
Otto, M.J.10
Furman, P.A.11
-
13
-
-
77957913871
-
Discovery of a β- D -2′-deoxy-2′-fluoro-2′-β- C -methyluridine nucleotide prodrug (PSI-7977) for the treatment of hepatitis C virus
-
Sofia, M. J.; Bao, D.; Chang, W.; Du, J.; Nagarathnam, D.; Rachakonda, S.; Reddy, P. G.; Ross, B. S.; Wang, P.; Zhang, H.-R.; Bansal, S.; Espiritu, C.; Keilman, M.; Lam, A. M.; Micolochick Steuer, H. M.; Niu, C.; Otto, M. J.; Furman, P. A. Discovery of a β- d -2′-deoxy-2′-fluoro-2′- β- C -methyluridine nucleotide prodrug (PSI-7977) for the treatment of hepatitis C virus J. Med. Chem. 2010, 53, 7202-7218
-
(2010)
J. Med. Chem.
, vol.53
, pp. 7202-7218
-
-
Sofia, M.J.1
Bao, D.2
Chang, W.3
Du, J.4
Nagarathnam, D.5
Rachakonda, S.6
Reddy, P.G.7
Ross, B.S.8
Wang, P.9
Zhang, H.-R.10
Bansal, S.11
Espiritu, C.12
Keilman, M.13
Lam, A.M.14
Micolochick Steuer, H.M.15
Niu, C.16
Otto, M.J.17
Furman, P.A.18
-
14
-
-
33747113565
-
Rational design of polymerase inhibitors as antiviral drugs
-
Oeberg, Bo. Rational design of polymerase inhibitors as antiviral drugs Antiviral Res. 2006, 71, 90-95
-
(2006)
Antiviral Res.
, vol.71
, pp. 90-95
-
-
Oeberg, Bo.1
-
15
-
-
43049112098
-
Prodrugs of phosphates and phosphonates
-
DOI 10.1021/jm701260b
-
Hecker, S. J.; Erion, M. D. Prodrugs of phosphates and phosphonates J. Med. Chem. 2008, 51, 2328-2345 (Pubitemid 351628494)
-
(2008)
Journal of Medicinal Chemistry
, vol.51
, Issue.8
, pp. 2328-2345
-
-
Hecker, S.J.1
Erion, M.D.2
-
16
-
-
73449119606
-
Aryloxy phosphoramidate triesters: A technology for delivering monophosphorylated nucleosides and sugars into cells
-
Mehellou, Y.; Balzarini, J.; McGuigan, C. Aryloxy phosphoramidate triesters: a technology for delivering monophosphorylated nucleosides and sugars into cells ChemMedChem 2009, 4, 1779-1791
-
(2009)
ChemMedChem
, vol.4
, pp. 1779-1791
-
-
Mehellou, Y.1
Balzarini, J.2
McGuigan, C.3
-
17
-
-
77955426384
-
Design, synthesis and evaluation of a novel double pro-drug: INX-08189. A new clinical candidate for hepatitis C virus
-
McGuigan, C.; Madela, K.; Aljarah, M.; Gilles, A.; Brancale, A.; Zonta, N.; Chamberlain, S.; Vernachio, J.; Hutchins, J.; Hall, A.; Ames, B.; Gorovits, E.; Ganguly, B.; Kolykhalov, A.; Wang, J.; Muhammad, J.; Patti, J. M.; Henson, G. Design, synthesis and evaluation of a novel double pro-drug: INX-08189. A new clinical candidate for hepatitis C virus Bioorg. Med. Chem. Lett. 2010, 20, 4850-4854
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 4850-4854
-
-
McGuigan, C.1
Madela, K.2
Aljarah, M.3
Gilles, A.4
Brancale, A.5
Zonta, N.6
Chamberlain, S.7
Vernachio, J.8
Hutchins, J.9
Hall, A.10
Ames, B.11
Gorovits, E.12
Ganguly, B.13
Kolykhalov, A.14
Wang, J.15
Muhammad, J.16
Patti, J.M.17
Henson, G.18
-
18
-
-
77954347956
-
Phosphoramidate ProTides of 2′-C-methylguanosine as highly potent inhibitors of hepatitis C virus. study of their in vitro and in vivo properties
-
McGuigan, C.; Gilles, A.; Madela, K.; Aljarah, M.; Holl, S.; Jones, S.; Vernachio, J.; Hutchins, J.; Ames, B.; Bryant, K. D.; Gorovits, E.; Ganguly, B.; Hunley, D.; Hall, A.; Kolykhalov, A.; Liu, Y.; Muhammad, J.; Raja, N.; Walters, R.; Wang, J.; Chamberlain, S.; Henson, G. Phosphoramidate ProTides of 2′-C-methylguanosine as highly potent inhibitors of hepatitis C virus. study of their in vitro and in vivo properties J. Med. Chem. 2010, 53, 4949-4957
-
(2010)
J. Med. Chem.
, vol.53
, pp. 4949-4957
-
-
McGuigan, C.1
Gilles, A.2
Madela, K.3
Aljarah, M.4
Holl, S.5
Jones, S.6
Vernachio, J.7
Hutchins, J.8
Ames, B.9
Bryant, K.D.10
Gorovits, E.11
Ganguly, B.12
Hunley, D.13
Hall, A.14
Kolykhalov, A.15
Liu, Y.16
Muhammad, J.17
Raja, N.18
Walters, R.19
Wang, J.20
Chamberlain, S.21
Henson, G.22
more..
-
19
-
-
69549122650
-
An efficient and diastereoselective synthesis of PSI-6130: A clinically efficacious inhibitor of HCV NS5B polymerase
-
Wang, P.; Chun, B.-K.; Rachakonda, S.; Du, J.; Khan, N.; Shi, J.; Stec, W.; Cleary, D.; Ross, B. S.; Sofia, M. J. An efficient and diastereoselective synthesis of PSI-6130: a clinically efficacious inhibitor of HCV NS5B polymerase J. Org. Chem. 2009, 74, 6819-6824
-
(2009)
J. Org. Chem.
, vol.74
, pp. 6819-6824
-
-
Wang, P.1
Chun, B.-K.2
Rachakonda, S.3
Du, J.4
Khan, N.5
Shi, J.6
Stec, W.7
Cleary, D.8
Ross, B.S.9
Sofia, M.J.10
-
20
-
-
79951526462
-
-
The improved synthesis of the intermediate 5 will be published elsewhere
-
The improved synthesis of the intermediate 5 will be published elsewhere.
-
-
-
-
21
-
-
33845350198
-
Application of phosphoramidate ProTide technology significantly improves antiviral potency of carbocyclic adenosine derivatives
-
DOI 10.1021/jm060776w
-
McGuigan, C.; Hassan-Abdallah, A.; Srinivasan, S.; Wang, Y.; Siddiqui, A.; Daluge, S. M.; Gudmundsson, K. S.; Zhou, H.; McLean, E. W.; Peckham, J. P.; Burnette, T. C.; Marr, H.; Hazen, R.; Condreay, L. D.; Johnson, L.; Balzarini, J. Application of phosphoramidate ProTide technology significantly improves the antiviral potency of carbocyclic adenosine derivatives J. Med. Chem. 2006, 49, 7215-7226 (Pubitemid 44886007)
-
(2006)
Journal of Medicinal Chemistry
, vol.49
, Issue.24
, pp. 7215-7226
-
-
McGuigan, C.1
Hassan-Abdallah, A.2
Srinivasan, S.3
Wang, Y.4
Siddiqui, A.5
Daluge, S.M.6
Gudmundsson, K.S.7
Zhou, H.8
McLean, E.W.9
Peckham, J.P.10
Burnette, T.C.11
Marr, H.12
Hazen, R.13
Condreay, L.D.14
Johnson, L.15
Balzarini, J.16
-
22
-
-
79951537996
-
-
In addition to l -alanine, other amino acid derivatives were also prepared and studied (no data shown). However, the phosphoramidates of l -alanine were strongly preferred to the others in terms of anti-HCV potency in vitro
-
In addition to l -alanine, other amino acid derivatives were also prepared and studied (no data shown). However, the phosphoramidates of l -alanine were strongly preferred to the others in terms of anti-HCV potency in vitro.
-
-
-
-
23
-
-
33947723257
-
Cyclic monophosphate prodrugs of base-modified 2′-C-methyl ribonucleosides as potent inhibitors of hepatitis C virus RNA replication
-
DOI 10.1016/j.bmcl.2007.02.030, PII S0960894X07002284
-
For previously reported 6-modified guanine nucleotide analogues with anti-HCV activity, see: Gunic, E.; Girardet, J.-L.; Ramasamy, K.; Stoisavljevic-Petkov, V.; Chow, S.; Yeh, L.-T.; Hamatake, R. K.; Raney, A.; Hong, Z. Cyclic monophosphate prodrugs of base-modified 2′- C -methyl ribonucleosides as potent inhibitors of hepatitis C virus RNA replication Bioorg. Med. Chem. Lett. 2007, 17, 2452-2455 (Pubitemid 46507791)
-
(2007)
Bioorganic and Medicinal Chemistry Letters
, vol.17
, Issue.9
, pp. 2452-2455
-
-
Gunic, E.1
Girardet, J.-L.2
Ramasamy, K.3
Stoisavljevic-Petkov, V.4
Chow, S.5
Yeh, L.-T.6
Hamatake, R.K.7
Raney, A.8
Hong, Z.9
-
24
-
-
0029127419
-
2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies
-
Lambe, C. U.; Averett, D. R.; Paff, M. T.; Reardon, J. E.; Wilson, J. G.; Krenitsky, T. A. 2-Amino-6-methoxypurine arabinoside: an agent for T-cell malignancies Cancer Res. 1995, 55, 3352-3356
-
(1995)
Cancer Res.
, vol.55
, pp. 3352-3356
-
-
Lambe, C.U.1
Averett, D.R.2
Paff, M.T.3
Reardon, J.E.4
Wilson, J.G.5
Krenitsky, T.A.6
-
26
-
-
75149151884
-
Resistance to direct antiviral agents in patients with hepatitis C virus infection
-
Sarrazin, C.; Zeuzem, S. Resistance to direct antiviral agents in patients with hepatitis C virus infection Gastroenterology 2010, 138, 447-462
-
(2010)
Gastroenterology
, vol.138
, pp. 447-462
-
-
Sarrazin, C.1
Zeuzem, S.2
-
27
-
-
24744436849
-
Cytostatic 6-arylpurine nucleosides. 6. SAR in anti-HCV and cytostatic activity of extended series of 6-hetarylpurine ribonucleosides
-
DOI 10.1021/jm050335x
-
Hocek, M.; Naus, P.; Pohl, R.; Votruba, I.; Furman, P. A.; Tharnish, P. M.; Otto, M. J. Cytostatic 6-arylpurine nucleosides. 6. SAR in anti-HCV and cytostatic activity of extended series of 6-hetarylpurine ribonucleosides J. Med. Chem. 2005, 48, 5869-5873 (Pubitemid 41298356)
-
(2005)
Journal of Medicinal Chemistry
, vol.48
, Issue.18
, pp. 5869-5873
-
-
Hocek, M.1
Naus, P.2
Pohl, R.3
Votruba, I.4
Furman, P.A.5
Tharnish, P.M.6
Otto, M.J.7
-
28
-
-
2342539175
-
Nucleoside analogues and mitochondrial toxicity
-
Fleischer, R.; Boxwell, D.; Sherman, K. E. Nucleoside analogues and mitochondrial toxicity Clin. Infect. Dis. 2004, 38, e79-80
-
(2004)
Clin. Infect. Dis.
, vol.38
, pp. 79-80
-
-
Fleischer, R.1
Boxwell, D.2
Sherman, K.E.3
-
29
-
-
35648968189
-
Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor β-D-2′-deoxy-2′-fluoro-2′-C- methylcytidine (PSI-6130) and identification of a novel active 5′-triphosphate species
-
DOI 10.1074/jbc.M705274200
-
Ma, H.; Jiang, W.-R.; Robledo, N.; Leveque, V.; Ali, S.; Lara-Jaime, T.; Masjedizadeh, M.; Smith, D. B.; Cammack, N.; Klumpp, K.; Symons, J. Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor β- d -2′-Deoxy-2′-fluoro-2′-C-methylcytidine (PSI-6130) and identification of a novel active 5′-triphosphate species J. Biol. Chem. 2007, 282, 29812-29820 (Pubitemid 350035263)
-
(2007)
Journal of Biological Chemistry
, vol.282
, Issue.41
, pp. 29812-29820
-
-
Ma, H.1
Jiang, W.-R.2
Robledo, N.3
Leveque, V.4
Ali, S.5
Lara-Jaime, T.6
Masjedizadeh, M.7
Smith, D.B.8
Cammack, N.9
Klumpp, K.10
Symons, J.11
-
30
-
-
79951523609
-
-
When compound 23 was prepared by the method described in the Supporting Information. The ratio varies depending on the reaction conditions. Selective synthetic preparation of 23b will be reported elsewhere in the near future.
-
When compound 23 was prepared by the method described in the Supporting Information. The ratio varies depending on the reaction conditions. Selective synthetic preparation of 23b will be reported elsewhere in the near future.
-
-
-
|