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Discovery of Ruzasvir (MK-8408): A Potent, Pan-Genotype HCV NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Polymorphisms.
Tong L, Yu W, Chen L, Selyutin O, Dwyer MP, Nair AG, Mazzola R, Kim JH, Sha D, Yin J, Ruck RT, Davies IW, Hu B, Zhong B, Hao J, Ji T, Zan S, Liu R, Agrawal S, Xia E, Curry S, McMonagle P, Bystol K, Lahser F, Carr D, Rokosz L, Ingravallo P, Chen S, Feng KI, Cartwright M, Asante-Appiah E, Kozlowski JA. Tong L, et al. Among authors: xia e. J Med Chem. 2017 Jan 12;60(1):290-306. doi: 10.1021/acs.jmedchem.6b01310. Epub 2016 Nov 15. J Med Chem. 2017. PMID: 27808515 Free article.
Discovery of fused tricyclic core containing HCV NS5A inhibitors with pan-genotype activity.
Yu W, Coburn CA, Yang DY, Meinke PT, Wong M, Rosenblum SB, Chen KX, Njoroge GF, Chen L, Dwyer MP, Jiang Y, Nair AG, Selyutin O, Tong L, Zeng Q, Zhong B, Ji T, Hu B, Agrawal S, Xia E, Zhai Y, Liu R, Kong R, Ingravallo P, Asante-Appiah E, Nomeir A, Fells J, Kozlowski JA. Yu W, et al. Among authors: xia e. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3158-3162. doi: 10.1016/j.bmcl.2016.04.084. Epub 2016 Apr 30. Bioorg Med Chem Lett. 2016. PMID: 27180013
Aryl or heteroaryl substituted aminal derivatives of HCV NS5A inhibitor MK-8742.
Yu W, Coburn CA, Nair AG, Wong M, Rosenblum SB, Zhou G, Dwyer MP, Tong L, Hu B, Zhong B, Hao J, Ji T, Zan S, Kim SH, Zeng Q, Selyutin O, Chen L, Masse F, Agrawal S, Liu R, Xia E, Zhai Y, Curry S, McMonagle P, Ingravallo P, Asante-Appiah E, Lin M, Kozlowski JA. Yu W, et al. Among authors: xia e. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3414-20. doi: 10.1016/j.bmcl.2016.06.056. Epub 2016 Jun 22. Bioorg Med Chem Lett. 2016. PMID: 27394665
Matched and mixed cap derivatives in the tetracyclic indole class of HCV NS5A inhibitors.
Dwyer MP, Keertikar KM, Chen L, Tong L, Selyutin O, Nair AG, Yu W, Zhou G, Lavey BJ, Yang DY, Wong M, Kim SH, Coburn CA, Rosenblum SB, Zeng Q, Jiang Y, Shankar BB, Rizvi R, Nomeir AA, Liu R, Agrawal S, Xia E, Kong R, Zhai Y, Ingravallo P, Asante-Appiah E, Kozlowski JA. Dwyer MP, et al. Among authors: xia e. Bioorg Med Chem Lett. 2016 Aug 15;26(16):4106-11. doi: 10.1016/j.bmcl.2016.06.063. Epub 2016 Jun 25. Bioorg Med Chem Lett. 2016. PMID: 27423481
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: xia e. 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
Alternative core development around the tetracyclic indole class of HCV NS5A inhibitors.
Tong L, Yu W, Coburn CA, Meinke PT, Nair AG, Dwyer MP, Chen L, Selyutin O, Rosenblum SB, Jiang Y, Fells J, Hu B, Zhong B, Soll RM, Liu R, Agrawal S, Xia E, Zhai Y, Kong R, Ingravallo P, Nomeir A, Asante-Appiah E, Kozlowski JA. Tong L, et al. Among authors: xia e. Bioorg Med Chem Lett. 2016 Oct 15;26(20):5132-5137. doi: 10.1016/j.bmcl.2016.07.057. Epub 2016 Jul 25. Bioorg Med Chem Lett. 2016. PMID: 27634194 Free article.
MK-8325: A silyl proline-containing NS5A inhibitor with pan-genotype activity for treatment of HCV.
Nair AG, Zeng Q, Selyutin O, Rosenblum SB, Jiang Y, Yang DY, Keertikar K, Zhou G, Dwyer M, Kim SH, Shankar B, Yu W, Tong L, Chen L, Mazzola R, Caldwell J, Tang H, Agrawal S, Liu R, Kong R, Ingravallo P, Xia E, Zhai Y, Nomeir A, Asante-Appiah E, Kozlowski JA. Nair AG, et al. Among authors: xia e. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1954-1957. doi: 10.1016/j.bmcl.2018.03.049. Epub 2018 Mar 20. Bioorg Med Chem Lett. 2018. PMID: 29653894
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: xia e. 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
The Combination of Grazoprevir, a Hepatitis C Virus (HCV) NS3/4A Protease Inhibitor, and Elbasvir, an HCV NS5A Inhibitor, Demonstrates a High Genetic Barrier to Resistance in HCV Genotype 1a Replicons.
Lahser FC, Bystol K, Curry S, McMonagle P, Xia E, Ingravallo P, Chase R, Liu R, Black T, Hazuda D, Howe AY, Asante-Appiah E. Lahser FC, et al. Among authors: xia e. Antimicrob Agents Chemother. 2016 Apr 22;60(5):2954-64. doi: 10.1128/AAC.00051-16. Print 2016 May. Antimicrob Agents Chemother. 2016. PMID: 26926625 Free PMC article.
364 results