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Page 1
Discovery of potent macrocyclic HCV NS5A inhibitors.
Yu W, Vibulbhan B, Rosenblum SB, Martin GS, Vellekoop AS, Holst CL, Coburn CA, Wong M, Selyutin O, Ji T, Zhong B, Hu B, Chen L, Dwyer MP, Jiang Y, Nair AG, Tong L, Zeng Q, Agrawal S, Carr D, Rokosz L, Liu R, Curry S, McMonagle P, Ingravallo P, Lahser F, Asante-Appiah E, Fells J, Kozlowski JA. Yu W, et al. Among authors: lahser f. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3793-9. doi: 10.1016/j.bmcl.2016.05.042. Epub 2016 May 17. Bioorg Med Chem Lett. 2016. PMID: 27282743
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: lahser f. 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
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: lahser f. 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 MK-6169, a Potent Pan-Genotype Hepatitis C Virus NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Substitutions.
Yu W, Tong L, Selyutin O, Chen L, Hu B, Zhong B, Hao J, Ji T, Zan S, Yin J, Ruck RT, Curry S, McMonagle P, Agrawal S, Rokosz L, Carr D, Ingravallo P, Bystol K, Lahser F, Liu R, Chen S, Feng KI, Cartwright M, Asante-Appiah E, Kozlowski JA. Yu W, et al. Among authors: lahser f. J Med Chem. 2018 May 10;61(9):3984-4003. doi: 10.1021/acs.jmedchem.7b01927. Epub 2018 May 1. J Med Chem. 2018. PMID: 29681153
Alkyl substituted aminal derivatives of HCV NS5A inhibitor MK-8742.
Yu W, Coburn CA, Nair AG, Wong M, Tong L, Dwyer MP, Hu B, Zhong B, Hao J, Yang DY, Selyutin O, Jiang Y, Rosenblum SB, Kim SH, Lavey BJ, Zhou G, Rizvi R, Shankar BB, Zeng Q, Chen L, Agrawal S, Carr D, Rokosz L, Liu R, Curry S, McMonagle P, Ingravallo P, Lahser F, Asante-Appiah E, Nomeir A, Kozlowski JA. Yu W, et al. Among authors: lahser f. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3800-5. doi: 10.1016/j.bmcl.2016.05.041. Epub 2016 May 14. Bioorg Med Chem Lett. 2016. PMID: 27282742
Discovery of 2-(4-sulfonamidophenyl)-indole 3-carboxamides as potent and selective inhibitors with broad hepatitis C virus genotype activity targeting HCV NS4B.
Zhang N, Turpoff A, Zhang X, Huang S, Liu Y, Almstead N, Njoroge FG, Gu Z, Graci J, Jung SP, Pichardo J, Colacino J, Lahser F, Ingravallo P, Weetall M, Nomeir A, Karp GM. Zhang N, et al. Among authors: lahser f. Bioorg Med Chem Lett. 2016 Jan 15;26(2):594-601. doi: 10.1016/j.bmcl.2015.11.065. Epub 2015 Nov 19. Bioorg Med Chem Lett. 2016. PMID: 26652483
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. Among authors: lahser f. 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.
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. 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.
32 results