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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: chen l, chen s. 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
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: chen l, chen s. 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 Chromane Containing Hepatitis C Virus (HCV) NS5A Inhibitors with Improved Potency against Resistance-Associated Variants.
Yu W, Tong L, Hu B, Zhong B, Hao J, Ji T, Zan S, Coburn CA, Selyutin O, Chen L, Rokosz L, Agrawal S, Liu R, Curry S, McMonagle P, Ingravallo P, Asante-Appiah E, Chen S, Kozlowski JA. Yu W, et al. Among authors: chen l, chen s. J Med Chem. 2016 Nov 23;59(22):10228-10243. doi: 10.1021/acs.jmedchem.6b01234. Epub 2016 Nov 9. J Med Chem. 2016. PMID: 27792320
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: chen l, chen s. 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.
Fused bi-heteroaryl substituted hydantoin compounds as TACE inhibitors.
Tong L, Kim SH, Rosner K, Yu W, Shankar BB, Chen L, Li D, Dai C, Girijavallabhan V, Popovici-Muller J, Yang L, Zhou G, Kosinski A, Siddiqui MA, Shih NY, Guo Z, Orth P, Chen S, Lundell D, Niu X, Umland S, Kozlowski JA. Tong L, et al. Among authors: chen l, chen s. Bioorg Med Chem Lett. 2017 Jul 15;27(14):3037-3042. doi: 10.1016/j.bmcl.2017.05.062. Epub 2017 May 22. Bioorg Med Chem Lett. 2017. PMID: 28558971
Development of a prodrug of hydantoin based TACE inhibitor.
Tong L, Kim SH, Chen L, Kosinski A, Shankar BB, Girijavallabhan V, Yang DY, Yu W, Zhou G, Shih NY, Chen S, Hu M, Lundell D, Niu X, Umland S, Kozlowski JA. Tong L, et al. Among authors: chen l, chen s. Bioorg Med Chem Lett. 2017 Aug 15;27(16):3704-3708. doi: 10.1016/j.bmcl.2017.07.007. Epub 2017 Jul 3. Bioorg Med Chem Lett. 2017. PMID: 28711352
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: chen l, chen s. 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
Structure and activity relationships of tartrate-based TACE inhibitors.
Li D, Popovici-Muller J, Belanger DB, Caldwell J, Dai C, David M, Girijavallabhan VM, Lavey BJ, Lee JF, Liu Z, Mazzola R, Rizvi R, Rosner KE, Shankar B, Spitler J, Ting PC, Vaccaro H, Yu W, Zhou G, Zhu Z, Niu X, Sun J, Guo Z, Orth P, Chen S, Kozlowski JA, Lundell DJ, Madison V, McKittrick B, Piwinski JJ, Shih NY, Shipps GW Jr, Siddiqui MA, Strickland CO. Li D, et al. Among authors: chen s. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4812-5. doi: 10.1016/j.bmcl.2010.06.104. Epub 2010 Jun 25. Bioorg Med Chem Lett. 2010. PMID: 20638281
2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors.
Dai C, Li D, Popovici-Muller J, Zhao L, Girijavallabhan VM, Rosner KE, Lavey BJ, Rizvi R, Shankar BB, Wong MK, Guo Z, Orth P, Strickland CO, Sun J, Niu X, Chen S, Kozlowski JA, Lundell DJ, Piwinski JJ, Shih NY, Siddiqui MA. Dai C, et al. Among authors: chen s. Bioorg Med Chem Lett. 2011 May 15;21(10):3172-6. doi: 10.1016/j.bmcl.2011.01.002. Epub 2011 Jan 6. Bioorg Med Chem Lett. 2011. PMID: 21458257
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