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Page 1
Structure-Property Basis for Solving Transporter-Mediated Efflux and Pan-Genotypic Inhibition in HCV NS5B Inhibitors.
Yeung KS, Beno BR, Mosure K, Zhu J, Grant-Young KA, Parcella K, Anjanappa P, Bora RO, Selvakumar K, Wang YK, Fang H, Krause R, Rigat K, Liu M, Lemm J, Sheriff S, Witmer M, Tredup J, Jardel A, Kish K, Parker D, Haskell R, Santone K, Meanwell NA, Soars MG, Roberts SB, Kadow JF. Yeung KS, et al. Among authors: haskell r. ACS Med Chem Lett. 2018 Nov 5;9(12):1217-1222. doi: 10.1021/acsmedchemlett.8b00379. eCollection 2018 Dec 13. ACS Med Chem Lett. 2018. PMID: 30613329 Free PMC article.
Discovery of a Hepatitis C Virus NS5B Replicase Palm Site Allosteric Inhibitor (BMS-929075) Advanced to Phase 1 Clinical Studies.
Yeung KS, Beno BR, Parcella K, Bender JA, Grant-Young KA, Nickel A, Gunaga P, Anjanappa P, Bora RO, Selvakumar K, Rigat K, Wang YK, Liu M, Lemm J, Mosure K, Sheriff S, Wan C, Witmer M, Kish K, Hanumegowda U, Zhuo X, Shu YZ, Parker D, Haskell R, Ng A, Gao Q, Colston E, Raybon J, Grasela DM, Santone K, Gao M, Meanwell NA, Sinz M, Soars MG, Knipe JO, Roberts SB, Kadow JF. Yeung KS, et al. Among authors: haskell r. J Med Chem. 2017 May 25;60(10):4369-4385. doi: 10.1021/acs.jmedchem.7b00328. Epub 2017 May 4. J Med Chem. 2017. PMID: 28430437 Clinical Trial.
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: haskell r. 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.
The Discovery of GSK3640254, a Next-Generation Inhibitor of HIV-1 Maturation.
Regueiro-Ren A, Sit SY, Chen Y, Chen J, Swidorski JJ, Liu Z, Venables BL, Sin N, Hartz RA, Protack T, Lin Z, Zhang S, Li Z, Wu DR, Li P, Kempson J, Hou X, Gupta A, Rampulla R, Mathur A, Park H, Sarjeant A, Benitex Y, Rahematpura S, Parker D, Phillips T, Haskell R, Jenkins S, Santone KS, Cockett M, Hanumegowda U, Dicker I, Meanwell NA, Krystal M. Regueiro-Ren A, et al. Among authors: haskell r. J Med Chem. 2022 Sep 22;65(18):11927-11948. doi: 10.1021/acs.jmedchem.2c00879. Epub 2022 Aug 31. J Med Chem. 2022. PMID: 36044257
Design, Synthesis, and SAR of C-3 Benzoic Acid, C-17 Triterpenoid Derivatives. Identification of the HIV-1 Maturation Inhibitor 4-((1 R,3a S,5a R,5b R,7a R,11a S,11b R,13a R,13b R)-3a-((2-(1,1-Dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1 H-cyclopenta[ a]chrysen-9-yl)benzoic Acid (GSK3532795, BMS-955176).
Regueiro-Ren A, Swidorski JJ, Liu Z, Chen Y, Sin N, Sit SY, Chen J, Venables BL, Zhu J, Nowicka-Sans B, Protack T, Lin Z, Terry B, Samanta H, Zhang S, Li Z, Easter J, Beno BR, Arora V, Huang XS, Rahematpura S, Parker DD, Haskell R, Santone KS, Cockett MI, Krystal M, Meanwell NA, Jenkins S, Hanumegowda U, Dicker IB. Regueiro-Ren A, et al. Among authors: haskell r. J Med Chem. 2018 Aug 23;61(16):7289-7313. doi: 10.1021/acs.jmedchem.8b00854. Epub 2018 Aug 1. J Med Chem. 2018. PMID: 30067361
Design and synthesis of 4-heteroaryl 1,2,3,4-tetrahydroisoquinolines as triple reuptake inhibitors.
Liu S, Zha C, Nacro K, Hu M, Cui W, Yang YL, Bhatt U, Sambandam A, Isherwood M, Yet L, Herr MT, Ebeltoft S, Hassler C, Fleming L, Pechulis AD, Payen-Fornicola A, Holman N, Milanowski D, Cotterill I, Mozhaev V, Khmelnitsky Y, Guzzo PR, Sargent BJ, Molino BF, Olson R, King D, Lelas S, Li YW, Johnson K, Molski T, Orie A, Ng A, Haskell R, Clarke W, Bertekap R, O'Connell J, Lodge N, Sinz M, Adams S, Zaczek R, Macor JE. Liu S, et al. Among authors: haskell r. ACS Med Chem Lett. 2014 May 13;5(7):760-5. doi: 10.1021/ml500053b. eCollection 2014 Jul 10. ACS Med Chem Lett. 2014. PMID: 25050161 Free PMC article.
Lipophilic salts of poorly soluble compounds to enable high-dose lipidic SEDDS formulations in drug discovery.
Morgen M, Saxena A, Chen XQ, Miller W, Nkansah R, Goodwin A, Cape J, Haskell R, Su C, Gudmundsson O, Hageman M, Kumar A, Chowan GS, Rao A, Holenarsipur VK. Morgen M, et al. Among authors: haskell r. Eur J Pharm Biopharm. 2017 Aug;117:212-223. doi: 10.1016/j.ejpb.2017.04.021. Epub 2017 Apr 21. Eur J Pharm Biopharm. 2017. PMID: 28438550 Free article.
118 results