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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: swidorski jj. 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
Preclinical Profile of the HIV-1 Maturation Inhibitor VH3739937.
McAuliffe B, Falk P, Chen J, Chen Y, Sit SY, Swidorski J, Hartz RA, Xu L, Venables B, Sin N, Meanwell NA, Regueiro-Ren A, Wensel D, Hanumegowda U, Krystal M. McAuliffe B, et al. Among authors: swidorski j. Viruses. 2024 Sep 24;16(10):1508. doi: 10.3390/v16101508. Viruses. 2024. PMID: 39459843 Free PMC article.
Atropisomerism Observed in Galactose-Based Monosaccharide Inhibitors of Galectin-3 Comprising 2-Methyl-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione.
Yoon DS, Liu C, Jalagam PR, Feng J, Wang W, Swidorski JJ, Xu L, Hartz RA, Nair SK, Beno BR, Panda M, Ghosh K, Kumar A, Sale H, Shah D, Mathur A, Ellsworth BA, Cheng D, Regueiro-Ren A. Yoon DS, et al. Among authors: swidorski jj. J Med Chem. 2024 Aug 22;67(16):14184-14199. doi: 10.1021/acs.jmedchem.4c01008. Epub 2024 Aug 5. J Med Chem. 2024. PMID: 39102502
Identification of benzothiazole derived monosaccharides as potent, selective, and orally bioavailable inhibitors of human and mouse galectin-3; a rare example of using a S···O binding interaction for drug design.
Liu C, Wang W, Feng J, Beno B, Raja T, Swidorski J, Manepalli RKVLP, Vetrichelvan M, Rao Jalagam P, Nair SK, Gupta A, Panda M, Ghosh K, Kaushikkumar Shukla J, Sale H, Shah D, Singh Gautam S, Patel D, Mathur A, Ellsworth BA, Cheng D, Regueiro-Ren A. Liu C, et al. Among authors: swidorski j. Bioorg Med Chem. 2024 Mar 1;101:117638. doi: 10.1016/j.bmc.2024.117638. Epub 2024 Feb 11. Bioorg Med Chem. 2024. PMID: 38394996
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: swidorski jj. 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 and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition.
Swidorski JJ, Jenkins S, Hanumegowda U, Parker DD, Beno BR, Protack T, Ng A, Gupta A, Shanmugam Y, Dicker IB, Krystal M, Meanwell NA, Regueiro-Ren A. Swidorski JJ, et al. Bioorg Med Chem Lett. 2021 Mar 15;36:127823. doi: 10.1016/j.bmcl.2021.127823. Epub 2021 Jan 26. Bioorg Med Chem Lett. 2021. PMID: 33508465
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: swidorski jj. 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
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: swidorski jj. 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
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: swidorski jj. 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.
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: swidorski jj. 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.
18 results