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Page 1
Discovery of an irreversible HCV NS5B polymerase inhibitor.
Zeng Q, Nair AG, Rosenblum SB, Huang HC, Lesburg CA, Jiang Y, Selyutin O, Chan TY, Bennett F, Chen KX, Venkatraman S, Sannigrahi M, Velazquez F, Duca JS, Gavalas S, Huang Y, Pu H, Wang L, Pinto P, Vibulbhan B, Agrawal S, Ferrari E, Jiang CK, Li C, Hesk D, Gesell J, Sorota S, Shih NY, Njoroge FG, Kozlowski JA. Zeng Q, et al. Among authors: li c. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6585-7. doi: 10.1016/j.bmcl.2013.10.060. Epub 2013 Nov 6. Bioorg Med Chem Lett. 2013. PMID: 24252545
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. Chen KX, et al. Among authors: li c. J Med Chem. 2012 Jan 26;55(2):754-65. doi: 10.1021/jm201258k. Epub 2012 Jan 6. J Med Chem. 2012. PMID: 22148957
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. Chen KX, et al. Among authors: li c. J Med Chem. 2012 Mar 8;55(5):2089-101. doi: 10.1021/jm201322r. Epub 2012 Feb 22. J Med Chem. 2012. PMID: 22247956
5-Benzothiazole substituted pyrimidine derivatives as HCV replication (replicase) inhibitors.
Arasappan A, Bennett F, Girijavallabhan V, Huang Y, Huelgas R, Alvarez C, Chen L, Gavalas S, Kim SH, Kosinski A, Pinto P, Rizvi R, Rossman R, Shankar B, Tong L, Velazquez F, Venkatraman S, Verma VA, Kozlowski J, Shih NY, Piwinski JJ, MacCoss M, Kwong CD, Clark JL, Fowler AT, Geng F, Kezar HS 3rd, Roychowdhury A, Reynolds RC, Maddry JA, Ananthan S, Secrist JA 3rd, Li C, Chase R, Curry S, Huang HC, Tong X, Njoroge FG. Arasappan A, et al. Among authors: li c. Bioorg Med Chem Lett. 2012 May 1;22(9):3229-34. doi: 10.1016/j.bmcl.2012.03.036. Epub 2012 Mar 13. Bioorg Med Chem Lett. 2012. PMID: 22472692
Pyridofuran substituted pyrimidine derivatives as HCV replication (replicase) inhibitors.
Bennett F, Kezar HS 3rd, Girijavallabhan V, Huang Y, Huelgas R, Rossman R, Shih NY, Piwinski JJ, MacCoss M, Kwong CD, Clark JL, Fowler AT, Geng F, Roychowdhury A, Reynolds RC, Maddry JA, Ananthan S, Secrist JA 3rd, Li C, Chase R, Curry S, Huang HC, Tong X, George Njoroge F, Arasappan A. Bennett F, et al. Among authors: li c. Bioorg Med Chem Lett. 2012 Aug 1;22(15):5144-9. doi: 10.1016/j.bmcl.2012.06.021. Epub 2012 Jun 19. Bioorg Med Chem Lett. 2012. PMID: 22814211
Synthesis and SAR of pyridothiazole substituted pyrimidine derived HCV replication inhibitors.
Girijavallabhan VM, Alvarez C, Bennett F, Chen L, Gavalas S, Huang Y, Kim SH, Kosinski A, Pinto P, Rizvi R, Rossman R, Shankar B, Tong L, Velazquez F, Venkatraman S, Verma VA, Kozlowski J, Shih NY, Piwinski JJ, MacCoss M, Kwong CD, Bansal N, Clark JL, Fowler AT, Kezar HS 3rd, Valiyaveettil J, Reynolds RC, Maddry JA, Ananthan S, Secrist JA 3rd, Li C, Chase R, Curry S, Huang HC, Tong X, Njoroge FG, Arasappan A. Girijavallabhan VM, et al. Among authors: li c. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5652-7. doi: 10.1016/j.bmcl.2012.06.099. Epub 2012 Jul 15. Bioorg Med Chem Lett. 2012. PMID: 22858143
Synthesis and SAR of geminal substitutions at the C5' carbosugar position of pyrimidine-derived HCV inhibitors.
Verma VA, Rossman R, Bennett F, Chen L, Gavalas S, Girijavallabhan V, Huang Y, Kim SH, Kosinski A, Pinto P, Rizvi R, Shankar B, Tong L, Velazquez F, Venkatraman S, Kozlowski J, MacCoss M, Kwong CD, Bansal N, Kezar HS 3rd, Reynolds RC, Maddry JA, Ananthan S, Secrist JA 3rd, Li C, Chase R, Curry S, Huang HC, Tong X, Njoroge FG, Arasappan A. Verma VA, et al. Among authors: li c. Bioorg Med Chem Lett. 2012 Nov 15;22(22):6967-73. doi: 10.1016/j.bmcl.2012.08.111. Epub 2012 Sep 7. Bioorg Med Chem Lett. 2012. PMID: 23036957
Discovery of novel tricyclic indole derived inhibitors of HCV NS5B RNA dependent RNA polymerase.
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, Huang HC, Agrawal S, Jiang CK, Ferrari E, Li C, Kozlowski J, Rosenblum S, Shih NY, Njoroge FG. Venkatraman S, et al. Among authors: li c. Bioorg Med Chem. 2013 Apr 1;21(7):2007-17. doi: 10.1016/j.bmc.2013.01.024. Epub 2013 Jan 23. Bioorg Med Chem. 2013. PMID: 23434368
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. Venkatraman S, et al. Among authors: li c. Bioorg Med Chem. 2014 Jan 1;22(1):447-58. doi: 10.1016/j.bmc.2013.11.007. Epub 2013 Nov 13. Bioorg Med Chem. 2014. PMID: 24275348
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. Chen KX, et al. Among authors: li c. ACS Med Chem Lett. 2013 Aug 12;5(3):244-8. doi: 10.1021/ml400192w. eCollection 2014 Mar 13. ACS Med Chem Lett. 2013. PMID: 24900812 Free PMC article.
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