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Page 1
Invention of VH-937, a Potent HIV-1 Maturation Inhibitor with the Potential for Infrequent Oral Dosing in Humans.
Sit SY, Chen Y, Chen J, Venables BL, Swidorski JJ, Xu L, Sin N, Hartz RA, Lin Z, Zhang S, Li Z, Wu DR, Li P, Kempson J, Hou X, Shanmugam Y, Parker D, Jenkins S, Simmermacher J, Falk P, McAuliffe B, Cockett M, Hanumegowda U, Dicker I, Krystal M, Meanwell NA, Regueiro-Ren A. Sit SY, et al. Among authors: chen j, chen y. ACS Med Chem Lett. 2024 Oct 17;15(11):1997-2004. doi: 10.1021/acsmedchemlett.4c00419. eCollection 2024 Nov 14. ACS Med Chem Lett. 2024. PMID: 39563829
Discovery and early clinical evaluation of BMS-605339, a potent and orally efficacious tripeptidic acylsulfonamide NS3 protease inhibitor for the treatment of hepatitis C virus infection.
Scola PM, Wang AX, Good AC, Sun LQ, Combrink KD, Campbell JA, Chen J, Tu Y, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D'Andrea S, Zheng B, Hewawasam P, Ding M, Thuring J, Li J, Hernandez D, Yu F, Falk P, Zhai G, Sheaffer AK, Chen C, Lee MS, Barry D, Knipe JO, Li W, Han YH, Jenkins S, Gesenberg C, Gao Q, Sinz MW, Santone KS, Zvyaga T, Rajamani R, Klei HE, Colonno RJ, Grasela DM, Hughes E, Chien C, Adams S, Levesque PC, Li D, Zhu J, Meanwell NA, McPhee F. Scola PM, et al. Among authors: chen j, chen c, chen y. J Med Chem. 2014 Mar 13;57(5):1708-29. doi: 10.1021/jm401840s. Epub 2014 Feb 20. J Med Chem. 2014. PMID: 24555570
The discovery of asunaprevir (BMS-650032), an orally efficacious NS3 protease inhibitor for the treatment of hepatitis C virus infection.
Scola PM, Sun LQ, Wang AX, Chen J, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D'Andrea SV, Zheng B, Hewawasam P, Tu Y, Friborg J, Falk P, Hernandez D, Levine S, Chen C, Yu F, Sheaffer AK, Zhai G, Barry D, Knipe JO, Han YH, Schartman R, Donoso M, Mosure K, Sinz MW, Zvyaga T, Good AC, Rajamani R, Kish K, Tredup J, Klei HE, Gao Q, Mueller L, Colonno RJ, Grasela DM, Adams SP, Loy J, Levesque PC, Sun H, Shi H, Sun L, Warner W, Li D, Zhu J, Meanwell NA, McPhee F. Scola PM, et al. Among authors: chen j, chen c, chen y. J Med Chem. 2014 Mar 13;57(5):1730-52. doi: 10.1021/jm500297k. Epub 2014 Mar 5. J Med Chem. 2014. PMID: 24564672
Inhibitors of HIV-1 maturation: Development of structure-activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids.
Swidorski JJ, Liu Z, Sit SY, Chen J, Chen Y, Sin N, Venables BL, Parker DD, Nowicka-Sans B, Terry BJ, Protack T, Rahematpura S, Hanumegowda U, Jenkins S, Krystal M, Dicker IB, Meanwell NA, Regueiro-Ren A. Swidorski JJ, et al. Among authors: chen j, chen y. Bioorg Med Chem Lett. 2016 Apr 15;26(8):1925-30. doi: 10.1016/j.bmcl.2016.03.019. Epub 2016 Mar 8. Bioorg Med Chem Lett. 2016. PMID: 26988305
Identification and Characterization of BMS-955176, a Second-Generation HIV-1 Maturation Inhibitor with Improved Potency, Antiviral Spectrum, and Gag Polymorphic Coverage.
Nowicka-Sans B, Protack T, Lin Z, Li Z, Zhang S, Sun Y, Samanta H, Terry B, Liu Z, Chen Y, Sin N, Sit SY, Swidorski JJ, Chen J, Venables BL, Healy M, Meanwell NA, Cockett M, Hanumegowda U, Regueiro-Ren A, Krystal M, Dicker IB. Nowicka-Sans B, et al. Among authors: chen j, chen y. Antimicrob Agents Chemother. 2016 Jun 20;60(7):3956-69. doi: 10.1128/AAC.02560-15. Print 2016 Jul. Antimicrob Agents Chemother. 2016. PMID: 27090171 Free PMC article.
Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity.
Regueiro-Ren A, Liu Z, Chen Y, Sin N, Sit SY, Swidorski JJ, Chen J, Venables BL, Zhu J, Nowicka-Sans B, Protack T, Lin Z, Terry B, Samanta H, Zhang S, Li Z, Beno BR, Huang XS, Rahematpura S, Parker DD, Haskell R, Jenkins S, Santone KS, Cockett MI, Krystal M, Meanwell NA, Hanumegowda U, Dicker IB. Regueiro-Ren A, et al. Among authors: chen j, chen y. ACS Med Chem Lett. 2016 Apr 22;7(6):568-72. doi: 10.1021/acsmedchemlett.6b00010. eCollection 2016 Jun 9. ACS Med Chem Lett. 2016. PMID: 27326328 Free PMC article.
Discovery of a Potent Acyclic, Tripeptidic, Acyl Sulfonamide Inhibitor of Hepatitis C Virus NS3 Protease as a Back-up to Asunaprevir with the Potential for Once-Daily Dosing.
Sun LQ, Mull E, Zheng B, D'Andrea S, Zhao Q, Wang AX, Sin N, Venables BL, Sit SY, Chen Y, Chen J, Cocuzza A, Bilder DM, Mathur A, Rampulla R, Chen BC, Palani T, Ganesan S, Arunachalam PN, Falk P, Levine S, Chen C, Friborg J, Yu F, Hernandez D, Sheaffer AK, Knipe JO, Han YH, Schartman R, Donoso M, Mosure K, Sinz MW, Zvyaga T, Rajamani R, Kish K, Tredup J, Klei HE, Gao Q, Ng A, Mueller L, Grasela DM, Adams S, Loy J, Levesque PC, Sun H, Shi H, Sun L, Warner W, Li D, Zhu J, Wang YK, Fang H, Cockett MI, Meanwell NA, McPhee F, Scola PM. Sun LQ, et al. Among authors: chen j, chen bc, chen c, chen y. J Med Chem. 2016 Sep 8;59(17):8042-60. doi: 10.1021/acs.jmedchem.6b00821. Epub 2016 Aug 26. J Med Chem. 2016. PMID: 27564532
Structure-activity relationships of 4-hydroxy-4-biaryl-proline acylsulfonamide tripeptides: A series of potent NS3 protease inhibitors for the treatment of hepatitis C virus.
Wang AX, Chen J, Zhao Q, Sun LQ, Friborg J, Yu F, Hernandez D, Good AC, Klei HE, Rajamani R, Mosure K, Knipe JO, Li D, Zhu J, Levesque PC, McPhee F, Meanwell NA, Scola PM. Wang AX, et al. Among authors: chen j. Bioorg Med Chem Lett. 2017 Feb 1;27(3):590-596. doi: 10.1016/j.bmcl.2016.12.013. Epub 2016 Dec 9. Bioorg Med Chem Lett. 2017. PMID: 28011221
Synthesis, Structure-Activity Relationships, and In Vivo Evaluation of Novel C-17 Amine Derivatives Based on GSK3640254 as HIV-1 Maturation Inhibitors with Broad Spectrum Activity.
Hartz RA, Xu L, Sit SY, Chen J, Venables BL, Lin Z, Zhang S, Li Z, Parker D, Simmons TS, Jenkins S, Hanumegowda UM, Dicker I, Krystal M, Meanwell NA, Regueiro-Ren A. Hartz RA, et al. Among authors: chen j. J Med Chem. 2022 Dec 8;65(23):15935-15966. doi: 10.1021/acs.jmedchem.2c01618. Epub 2022 Nov 28. J Med Chem. 2022. PMID: 36441509
Heterocyclic aminopyrrolidine derivatives as melatoninergic agents.
Sun LQ, Chen J, Mattson RJ, Epperson JR, Deskus JA, Li WS, Takaki K, Hodges DB, Iben L, Mahle CD, Ortiz A, Molstad D, Ryan E, Yeleswaram K, Xu C, Luo G. Sun LQ, et al. Among authors: chen j. Bioorg Med Chem Lett. 2003 Dec 15;13(24):4381-4. doi: 10.1016/j.bmcl.2003.09.030. Bioorg Med Chem Lett. 2003. PMID: 14643330
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