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Page 1
Antiviral activity, pharmacokinetics, and safety of BMS-488043, a novel oral small-molecule HIV-1 attachment inhibitor, in HIV-1-infected subjects.
Hanna GJ, Lalezari J, Hellinger JA, Wohl DA, Nettles R, Persson A, Krystal M, Lin P, Colonno R, Grasela DM. Hanna GJ, et al. Among authors: lin p. Antimicrob Agents Chemother. 2011 Feb;55(2):722-8. doi: 10.1128/AAC.00759-10. Epub 2010 Nov 15. Antimicrob Agents Chemother. 2011. PMID: 21078951 Free PMC article. Clinical Trial.
In vivo patterns of resistance to the HIV attachment inhibitor BMS-488043.
Zhou N, Nowicka-Sans B, Zhang S, Fan L, Fang J, Fang H, Gong YF, Eggers B, Langley DR, Wang T, Kadow J, Grasela D, Hanna GJ, Alexander L, Colonno R, Krystal M, Lin PF. Zhou N, et al. Antimicrob Agents Chemother. 2011 Feb;55(2):729-37. doi: 10.1128/AAC.01173-10. Epub 2010 Nov 15. Antimicrob Agents Chemother. 2011. PMID: 21078948 Free PMC article. Clinical Trial.
In vitro antiviral characteristics of HIV-1 attachment inhibitor BMS-626529, the active component of the prodrug BMS-663068.
Nowicka-Sans B, Gong YF, McAuliffe B, Dicker I, Ho HT, Zhou N, Eggers B, Lin PF, Ray N, Wind-Rotolo M, Zhu L, Majumdar A, Stock D, Lataillade M, Hanna GJ, Matiskella JD, Ueda Y, Wang T, Kadow JF, Meanwell NA, Krystal M. Nowicka-Sans B, et al. Antimicrob Agents Chemother. 2012 Jul;56(7):3498-507. doi: 10.1128/AAC.00426-12. Epub 2012 Apr 30. Antimicrob Agents Chemother. 2012. PMID: 22547625 Free PMC article.
A small molecule HIV-1 inhibitor that targets the HIV-1 envelope and inhibits CD4 receptor binding.
Lin PF, Blair W, Wang T, Spicer T, Guo Q, Zhou N, Gong YF, Wang HG, Rose R, Yamanaka G, Robinson B, Li CB, Fridell R, Deminie C, Demers G, Yang Z, Zadjura L, Meanwell N, Colonno R. Lin PF, et al. Proc Natl Acad Sci U S A. 2003 Sep 16;100(19):11013-8. doi: 10.1073/pnas.1832214100. Epub 2003 Aug 20. Proc Natl Acad Sci U S A. 2003. PMID: 12930892 Free PMC article.
Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug candidate that demonstrates antiviral activity in HIV-1-infected subjects.
Wang T, Yin Z, Zhang Z, Bender JA, Yang Z, Johnson G, Yang Z, Zadjura LM, D'Arienzo CJ, DiGiugno Parker D, Gesenberg C, Yamanaka GA, Gong YF, Ho HT, Fang H, Zhou N, McAuliffe BV, Eggers BJ, Fan L, Nowicka-Sans B, Dicker IB, Gao Q, Colonno RJ, Lin PF, Meanwell NA, Kadow JF. Wang T, et al. J Med Chem. 2009 Dec 10;52(23):7778-87. doi: 10.1021/jm900843g. J Med Chem. 2009. PMID: 19769332
Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 6. Preclinical and human pharmacokinetic profiling of BMS-663749, a phosphonooxymethyl prodrug of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)-2-oxoethanone (BMS-488043).
Kadow JF, Ueda Y, Meanwell NA, Connolly TP, Wang T, Chen CP, Yeung KS, Zhu J, Bender JA, Yang Z, Parker D, Lin PF, Colonno RJ, Mathew M, Morgan D, Zheng M, Chien C, Grasela D. Kadow JF, et al. Among authors: lin pf. J Med Chem. 2012 Mar 8;55(5):2048-56. doi: 10.1021/jm201218m. Epub 2012 Feb 22. J Med Chem. 2012. PMID: 22356441 Clinical Trial.
Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 12. Structure-activity relationships associated with 4-fluoro-6-azaindole derivatives leading to the identification of 1-(4-benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1h-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-585248).
Regueiro-Ren A, Xue QM, Swidorski JJ, Gong YF, Mathew M, Parker DD, Yang Z, Eggers B, D'Arienzo C, Sun Y, Malinowski J, Gao Q, Wu D, Langley DR, Colonno RJ, Chien C, Grasela DM, Zheng M, Lin PF, Meanwell NA, Kadow JF. Regueiro-Ren A, et al. J Med Chem. 2013 Feb 28;56(4):1656-69. doi: 10.1021/jm3016377. Epub 2013 Feb 7. J Med Chem. 2013. PMID: 23360431
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