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Page 1
Structure-activity relationships of proline modifications around the tetracyclic-indole class of NS5A inhibitors.
Tong L, Yu W, Coburn CA, Chen L, Selyutin O, Zeng Q, Dwyer MP, Nair AG, Shankar BB, Kim SH, Yang DY, Rosenblum SB, Ruck RT, Davies IW, Hu B, Zhong B, Hao J, Ji T, Zan S, Liu R, Agrawal S, Carr D, Curry S, McMonagle P, Bystol K, Lahser F, Ingravallo P, Chen S, Asante-Appiah E, Kozlowski JA. Tong L, et al. Among authors: zeng q. Bioorg Med Chem Lett. 2016 Nov 1;26(21):5354-5360. doi: 10.1016/j.bmcl.2016.08.097. Epub 2016 Sep 2. Bioorg Med Chem Lett. 2016. PMID: 27680588
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: zeng q. 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: zeng q. 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: zeng q. 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: zeng q. J Med Chem. 2012 Mar 8;55(5):2089-101. doi: 10.1021/jm201322r. Epub 2012 Feb 22. J Med Chem. 2012. PMID: 22247956
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: zeng q. 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
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. 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
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: zeng q. 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
IV. Discovery of CXCR3 antagonists substituted with heterocycles as amide surrogates: improved PK, hERG and metabolic profiles.
Nair AG, Wong MK, Shu Y, Jiang Y, Jenh CH, Kim SH, Yang DY, Zeng Q, Shao Y, Zawacki LG, Duo J, McGuinness BF, Carroll CD, Hobbs DW, Shih NY, Rosenblum SB, Kozlowski JA. Nair AG, et al. Among authors: zeng q. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1085-8. doi: 10.1016/j.bmcl.2014.01.009. Epub 2014 Jan 11. Bioorg Med Chem Lett. 2014. PMID: 24486132
Discovery of silyl proline containing HCV NS5A inhibitors with pan-genotype activity: SAR development.
Nair AG, Zeng Q, Selyutin O, Rosenblum SB, Jiang Y, Yang DY, Keertikar K, Zhou G, Dwyer MP, Kim SH, Shankar B, Yu W, Tong L, Chen L, Mazzola R, Caldwell J, Tang H, Allard ML, Buckle RN, Gauuan PJ, Holst CL, Martin GS, Naicker KP, Vellekoop S, Agrawal S, Liu R, Kong R, Ingravallo P, Xia E, Zhai Y, Nomeir A, Kozlowski JA. Nair AG, et al. Among authors: zeng q. Bioorg Med Chem Lett. 2016 Mar 1;26(5):1475-9. doi: 10.1016/j.bmcl.2016.01.050. Epub 2016 Jan 19. Bioorg Med Chem Lett. 2016. PMID: 26850003
7,720 results