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2018 2
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Page 1
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: rahematpura s. 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
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: rahematpura s. 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 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: rahematpura s. 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.
C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1 maturation inhibitors.
Liu Z, Swidorski JJ, Nowicka-Sans B, Terry B, Protack T, Lin Z, Samanta H, Zhang S, Li Z, Parker DD, Rahematpura S, Jenkins S, Beno BR, Krystal M, Meanwell NA, Dicker IB, Regueiro-Ren A. Liu Z, et al. Among authors: rahematpura s. Bioorg Med Chem. 2016 Apr 15;24(8):1757-70. doi: 10.1016/j.bmc.2016.03.001. Epub 2016 Mar 2. Bioorg Med Chem. 2016. PMID: 26968652
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: rahematpura s. 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
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: rahematpura s. 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 human immunodeficiency virus type 1 (HIV-1) attachment 13. Synthesis and profiling of a novel amminium prodrug of the HIV-1 attachment inhibitor BMS-585248.
Regueiro-Ren A, Simmermacher-Mayer J, Sinz M, Johnson KA, Huang XS, Jenkins S, Parker D, Rahematpura S, Zheng M, Meanwell NA, Kadow JF. Regueiro-Ren A, et al. Among authors: rahematpura s. J Med Chem. 2013 Feb 28;56(4):1670-6. doi: 10.1021/jm301638a. Epub 2013 Feb 12. J Med Chem. 2013. PMID: 23374053
The impact of P-glycoprotein on the disposition of drugs targeted for indications of the central nervous system: evaluation using the MDR1A/1B knockout mouse model.
Doran A, Obach RS, Smith BJ, Hosea NA, Becker S, Callegari E, Chen C, Chen X, Choo E, Cianfrogna J, Cox LM, Gibbs JP, Gibbs MA, Hatch H, Hop CE, Kasman IN, Laperle J, Liu J, Liu X, Logman M, Maclin D, Nedza FM, Nelson F, Olson E, Rahematpura S, Raunig D, Rogers S, Schmidt K, Spracklin DK, Szewc M, Troutman M, Tseng E, Tu M, Van Deusen JW, Venkatakrishnan K, Walens G, Wang EQ, Wong D, Yasgar AS, Zhang C. Doran A, et al. Among authors: rahematpura s. Drug Metab Dispos. 2005 Jan;33(1):165-74. doi: 10.1124/dmd.104.001230. Epub 2004 Oct 22. Drug Metab Dispos. 2005. PMID: 15502009
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