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Page 1
Substituted tetracyclic indole core derivatives of HCV NS5A inhibitor MK-8742.
Yu W, Zhou G, Coburn CA, Zeng Q, Tong L, Dwyer MP, Hu B, Zhong B, Hao J, Ji T, Zan S, Chen L, Mazzola R, Kim JH, Sha D, Selyutin O, Rosenblum SB, Lavey B, Nair AG, Heon Kim S, Keertikar KM, Rokosz L, Agrawal S, Liu R, Xia E, Zhai Y, Curry S, McMonagle P, Ingravallo P, Asante-Appiah E, Chen S, Kozlowski JA. Yu W, et al. Among authors: kozlowski ja. Bioorg Med Chem Lett. 2016 Oct 1;26(19):4851-4856. doi: 10.1016/j.bmcl.2016.08.002. Epub 2016 Aug 2. Bioorg Med Chem Lett. 2016. PMID: 27568086
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. 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. 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
In Vitro Antiviral Profile of Ruzasvir, a Potent and Pangenotype Inhibitor of Hepatitis C Virus NS5A.
Asante-Appiah E, Liu R, Curry S, McMonagle P, Agrawal S, Carr D, Rokosz L, Lahser F, Bystol K, Chase R, Black S, Ferrari E, Ingravallo P, Tong L, Yu W, Kozlowski J. Asante-Appiah E, et al. Antimicrob Agents Chemother. 2018 Oct 24;62(11):e01280-18. doi: 10.1128/AAC.01280-18. Print 2018 Nov. Antimicrob Agents Chemother. 2018. PMID: 30150466 Free PMC article.
Discovery of MK-8742: an HCV NS5A inhibitor with broad genotype activity.
Coburn CA, Meinke PT, Chang W, Fandozzi CM, Graham DJ, Hu B, Huang Q, Kargman S, Kozlowski J, Liu R, McCauley JA, Nomeir AA, Soll RM, Vacca JP, Wang D, Wu H, Zhong B, Olsen DB, Ludmerer SW. Coburn CA, et al. Among authors: kozlowski j. ChemMedChem. 2013 Dec;8(12):1930-40. doi: 10.1002/cmdc.201300343. Epub 2013 Oct 14. ChemMedChem. 2013. PMID: 24127258
Biaryl substituted hydantoin compounds as TACE inhibitors.
Yu W, Tong L, Kim SH, Wong MK, Chen L, Yang DY, Shankar BB, Lavey BJ, Zhou G, Kosinski A, Rizvi R, Li D, Feltz RJ, Piwinski JJ, Rosner KE, Shih NY, Siddiqui MA, Guo Z, Orth P, Shah H, Sun J, Umland S, Lundell DJ, Niu X, Kozlowski JA. Yu W, et al. Among authors: kozlowski ja. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5286-9. doi: 10.1016/j.bmcl.2010.06.134. Epub 2010 Jul 1. Bioorg Med Chem Lett. 2010. PMID: 20663669
I. Novel HCV NS5B polymerase inhibitors: discovery of indole 2-carboxylic acids with C3-heterocycles.
Anilkumar GN, Lesburg CA, Selyutin O, Rosenblum SB, Zeng Q, Jiang Y, Chan TY, Pu H, Vaccaro H, Wang L, Bennett F, Chen KX, Duca J, Gavalas S, Huang Y, Pinto P, Sannigrahi M, Velazquez F, Venkatraman S, Vibulbhan B, Agrawal S, Butkiewicz N, Feld B, Ferrari E, He Z, Jiang CK, Palermo RE, McMonagle P, Huang HC, Shih NY, Njoroge G, Kozlowski JA. Anilkumar GN, et al. Among authors: kozlowski ja. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5336-41. doi: 10.1016/j.bmcl.2011.07.021. Epub 2011 Jul 19. Bioorg Med Chem Lett. 2011. PMID: 21840715
II. Novel HCV NS5B polymerase inhibitors: discovery of indole C2 acyl sulfonamides.
Anilkumar GN, Selyutin O, Rosenblum SB, Zeng Q, Jiang Y, Chan TY, Pu H, Wang L, Bennett F, Chen KX, Lesburg CA, Duca J, Gavalas S, Huang Y, Pinto P, Sannigrahi M, Velazquez F, Venkatraman S, Vibulbhan B, Agrawal S, Ferrari E, Jiang CK, Huang HC, Shih NY, George Njoroge F, Kozlowski JA. Anilkumar GN, et al. Among authors: kozlowski ja. Bioorg Med Chem Lett. 2012 Jan 1;22(1):713-7. doi: 10.1016/j.bmcl.2011.10.041. Epub 2011 Oct 20. Bioorg Med Chem Lett. 2012. PMID: 22104146
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: kozlowski ja. 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: kozlowski ja. J Med Chem. 2012 Mar 8;55(5):2089-101. doi: 10.1021/jm201322r. Epub 2012 Feb 22. J Med Chem. 2012. PMID: 22247956
96 results