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Items: 1 to 20 of 90

1.

Discovery of SCH 900188: A Potent Hepatitis C Virus NS5B Polymerase Inhibitor Prodrug As a Development Candidate.

Chen KX, Venkatraman S, Anilkumar GN, Zeng Q, Lesburg CA, Vibulbhan B, Velazquez F, Chan TY, Bennet F, Jiang Y, Pinto P, Huang Y, Selyutin O, Agrawal S, Huang HC, Li C, Cheng KC, Shih NY, Kozlowski JA, Rosenblum SB, Njoroge FG.

ACS Med Chem Lett. 2013 Aug 12;5(3):244-8. doi: 10.1021/ml400192w. eCollection 2014 Mar 13.

2.

Structure-activity relationship (SAR) development and discovery of potent indole-based inhibitors of the hepatitis C virus (HCV) NS5B polymerase.

Chen KX, Vibulbhan B, Yang W, Sannigrahi M, Velazquez F, Chan TY, Venkatraman S, Anilkumar GN, Zeng Q, Bennet F, Jiang Y, Lesburg CA, Duca J, Pinto P, Gavalas S, Huang Y, Wu W, Selyutin O, Agrawal S, Feld B, Huang HC, Li C, Cheng KC, Shih NY, Kozlowski JA, Rosenblum SB, Njoroge FG.

J Med Chem. 2012 Jan 26;55(2):754-65. doi: 10.1021/jm201258k. Epub 2012 Jan 6.

PMID:
22148957
3.

Chemical genetics-based discovery of indole derivatives as HCV NS5B polymerase inhibitors.

Jin G, Lee S, Choi M, Son S, Kim GW, Oh JW, Lee C, Lee K.

Eur J Med Chem. 2014 Mar 21;75:413-25. doi: 10.1016/j.ejmech.2014.01.062. Epub 2014 Jan 31.

PMID:
24561671
4.

Tetracyclic indole inhibitors of hepatitis C virus NS5B-polymerase.

Stansfield I, Ercolani C, Mackay A, Conte I, Pompei M, Koch U, Gennari N, Giuliano C, Rowley M, Narjes F.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):627-32. doi: 10.1016/j.bmcl.2008.12.068. Epub 2008 Dec 24.

PMID:
19131244
5.

Screening of hepatitis C NS5B polymerase inhibitors containing benzothiadiazine core: a steered molecular dynamics.

Nutho B, Meeprasert A, Chulapa M, Kungwan N, Rungrotmongkol T.

J Biomol Struct Dyn. 2017 Jun;35(8):1743-1757. doi: 10.1080/07391102.2016.1193444. Epub 2016 Jun 27.

PMID:
27236925
6.

Optimization of potency and pharmacokinetics of tricyclic indole derived inhibitors of HCV NS5B polymerase. Identification of ester prodrugs with improved oral pharmacokinetics.

Venkatraman S, Velazquez F, Gavalas S, Wu W, Chen KX, Nair AG, Bennett F, Huang Y, Pinto P, Jiang Y, Selyutin O, Vibulbhan B, Zeng Q, Lesburg C, Duca J, Heimark L, Huang HC, Agrawal S, Jiang CK, Ferrari E, Li C, Kozlowski J, Rosenblum S, Shih NY, Njoroge FG.

Bioorg Med Chem. 2014 Jan 1;22(1):447-58. doi: 10.1016/j.bmc.2013.11.007. Epub 2013 Nov 13.

PMID:
24275348
7.

Structure-based virtual screening, synthesis and SAR of novel inhibitors of hepatitis C virus NS5B polymerase.

Talele TT, Arora P, Kulkarni SS, Patel MR, Singh S, Chudayeu M, Kaushik-Basu N.

Bioorg Med Chem. 2010 Jul 1;18(13):4630-8. doi: 10.1016/j.bmc.2010.05.030. Epub 2010 May 15.

8.
9.

Discovery of BI 207524, an indole diamide NS5B thumb pocket 1 inhibitor with improved potency for the potential treatment of chronic hepatitis C virus infection.

Beaulieu PL, Anderson PC, Bethell R, Bös M, Bousquet Y, Brochu C, Cordingley MG, Fazal G, Garneau M, Gillard JR, Kawai S, Marquis M, McKercher G, Poupart MA, Stammers T, Thavonekham B, Wernic D, Duan J, Kukolj G.

J Med Chem. 2014 Dec 11;57(23):10130-43. doi: 10.1021/jm501532z. Epub 2014 Nov 25.

PMID:
25393851
10.

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.

11.

Discovery of Novel Hepatitis C Virus NS5B Polymerase Inhibitors by Combining Random Forest, Multiple e-Pharmacophore Modeling and Docking.

Wei Y, Li J, Qing J, Huang M, Wu M, Gao F, Li D, Hong Z, Kong L, Huang W, Lin J.

PLoS One. 2016 Feb 4;11(2):e0148181. doi: 10.1371/journal.pone.0148181. eCollection 2016.

12.

Discovery of the first C-nucleoside HCV polymerase inhibitor (GS-6620) with demonstrated antiviral response in HCV infected patients.

Cho A, Zhang L, Xu J, Lee R, Butler T, Metobo S, Aktoudianakis V, Lew W, Ye H, Clarke M, Doerffler E, Byun D, Wang T, Babusis D, Carey AC, German P, Sauer D, Zhong W, Rossi S, Fenaux M, McHutchison JG, Perry J, Feng J, Ray AS, Kim CU.

J Med Chem. 2014 Mar 13;57(5):1812-25. doi: 10.1021/jm400201a. Epub 2013 May 1.

PMID:
23547794
13.

Discovery of HCV NS5B thumb site I inhibitors: core-refining from benzimidazole to indole scaffold.

Zhao F, Liu N, Zhan P, Jiang X, Liu X.

Eur J Med Chem. 2015 Apr 13;94:218-28. doi: 10.1016/j.ejmech.2015.03.012. Epub 2015 Mar 6. Review.

PMID:
25768704
14.

Interference of HCV replication by cell penetrable human monoclonal scFv specific to NS5B polymerase.

Thueng-in K, Thanongsaksrikul J, Jittavisutthikul S, Seesuay W, Chulanetra M, Sakolvaree Y, Srimanote P, Chaicumpa W.

MAbs. 2014;6(5):1327-39. doi: 10.4161/mabs.29978.

15.

Design and synthesis of imidazole N-H substituted amide prodrugs as inhibitors of hepatitis C virus replication.

Zong X, Cai J, Chen J, Wang P, Zhou G, Chen B, Li W, Ji M.

Bioorg Med Chem Lett. 2015 Aug 15;25(16):3147-50. doi: 10.1016/j.bmcl.2015.06.006. Epub 2015 Jun 9.

PMID:
26077493
16.

Discovery of new scaffolds for rational design of HCV NS5B polymerase inhibitors.

Golub AG, Gurukumar KR, Basu A, Bdzhola VG, Bilokin Y, Yarmoluk SM, Lee JC, Talele TT, Nichols DB, Kaushik-Basu N.

Eur J Med Chem. 2012 Dec;58:258-64. doi: 10.1016/j.ejmech.2012.09.010. Epub 2012 Sep 17.

17.

Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.

Cummings MD, Lin TI, Hu L, Tahri A, McGowan D, Amssoms K, Last S, Devogelaere B, Rouan MC, Vijgen L, Berke JM, Dehertogh P, Fransen E, Cleiren E, van der Helm L, Fanning G, Nyanguile O, Simmen K, Van Remoortere P, Raboisson P, Vendeville S.

J Med Chem. 2014 Mar 13;57(5):1880-92. doi: 10.1021/jm401396p. Epub 2013 Nov 8.

PMID:
24144360
18.

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.

19.

Synthesis of 2'-O,4'-C-alkylene-bridged ribonucleosides and their evaluation as inhibitors of HCV NS5B polymerase.

Chapron C, Glen R, La Colla M, Mayes BA, McCarville JF, Moore S, Moussa A, Sarkar R, Seifer M, Serra I, Stewart A.

Bioorg Med Chem Lett. 2014 Jun 15;24(12):2699-702. doi: 10.1016/j.bmcl.2014.04.050. Epub 2014 Apr 19.

PMID:
24815510
20.

A novel class of highly potent irreversible hepatitis C virus NS5B polymerase inhibitors.

Chen KX, Lesburg CA, Vibulbhan B, Yang W, Chan TY, Venkatraman S, Velazquez F, Zeng Q, Bennett F, Anilkumar GN, Duca J, Jiang Y, Pinto P, Wang L, Huang Y, Selyutin O, Gavalas S, Pu H, Agrawal S, Feld B, Huang HC, Li C, Cheng KC, Shih NY, Kozlowski JA, Rosenblum SB, Njoroge FG.

J Med Chem. 2012 Mar 8;55(5):2089-101. doi: 10.1021/jm201322r. Epub 2012 Feb 22.

PMID:
22247956

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