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The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation.
Chen Y, Sit SY, Chen J, Swidorski JJ, Liu Z, Sin N, Venables BL, Parker DD, Nowicka-Sans B, Lin Z, Li Z, Terry BJ, Protack T, Rahematpura S, Hanumegowda U, Jenkins S, Krystal M, Dicker ID, Meanwell NA, Regueiro-Ren A. Chen Y, et al. Among authors: liu z. Bioorg Med Chem Lett. 2018 May 15;28(9):1550-1557. doi: 10.1016/j.bmcl.2018.03.067. Epub 2018 Mar 26. Bioorg Med Chem Lett. 2018. PMID: 29631960
Inhibitors of HIV-1 attachment: The discovery and structure-activity relationships of tetrahydroisoquinolines as replacements for the piperazine benzamide in the 3-glyoxylyl 6-azaindole pharmacophore.
Swidorski JJ, Liu Z, Yin Z, Wang T, Carini DJ, Rahematpura S, Zheng M, Johnson K, Zhang S, Lin PF, Parker DD, Li W, Meanwell NA, Hamann LG, Regueiro-Ren A. Swidorski JJ, et al. Among authors: liu z. Bioorg Med Chem Lett. 2016 Jan 1;26(1):160-7. doi: 10.1016/j.bmcl.2015.11.009. Epub 2015 Nov 5. Bioorg Med Chem Lett. 2016. PMID: 26584882
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: liu z. 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: liu z. 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: liu z. 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.
Mechanistic Studies and Modeling Reveal the Origin of Differential Inhibition of Gag Polymorphic Viruses by HIV-1 Maturation Inhibitors.
Lin Z, Cantone J, Lu H, Nowicka-Sans B, Protack T, Yuan T, Yang H, Liu Z, Drexler D, Regueiro-Ren A, Meanwell NA, Cockett M, Krystal M, Lataillade M, Dicker IB. Lin Z, et al. Among authors: liu z. PLoS Pathog. 2016 Nov 28;12(11):e1005990. doi: 10.1371/journal.ppat.1005990. eCollection 2016 Nov. PLoS Pathog. 2016. PMID: 27893830 Free PMC article.
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: liu z. 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
Discovery of the Selective Protein Kinase C-θ Kinase Inhibitor, CC-90005.
Papa P, Whitefield B, Mortensen DS, Cashion D, Huang D, Torres E, Parnes J, Sapienza J, Hansen J, Correa M, Delgado M, Harris R, Hegde S, Norris S, Bahmanyar S, Plantevin-Krenitsky V, Liu Z, Leftheris K, Kulkarni A, Bennett B, Hur EM, Ringheim G, Khambatta G, Chan H, Muir J, Blease K, Burnett K, LeBrun L, Morrison L, Celeridad M, Khattri R, Cathers BE. Papa P, et al. Among authors: liu z. J Med Chem. 2021 Aug 26;64(16):11886-11903. doi: 10.1021/acs.jmedchem.1c00388. Epub 2021 Aug 6. J Med Chem. 2021. PMID: 34355886
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: liu z. 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
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