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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. Among authors: lin pf. J Med Chem. 2009 Dec 10;52(23):7778-87. doi: 10.1021/jm900843g. J Med Chem. 2009. PMID: 19769332
Biochemical and genetic characterizations of a novel human immunodeficiency virus type 1 inhibitor that blocks gp120-CD4 interactions.
Guo Q, Ho HT, Dicker I, Fan L, Zhou N, Friborg J, Wang T, McAuliffe BV, Wang HG, Rose RE, Fang H, Scarnati HT, Langley DR, Meanwell NA, Abraham R, Colonno RJ, Lin PF. Guo Q, et al. Among authors: lin pf. J Virol. 2003 Oct;77(19):10528-36. doi: 10.1128/jvi.77.19.10528-10536.2003. J Virol. 2003. PMID: 12970437 Free PMC article.
Discovery of 4-benzoyl-1-[(4-methoxy-1H- pyrrolo[2,3-b]pyridin-3-yl)oxoacetyl]-2- (R)-methylpiperazine (BMS-378806): a novel HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions.
Wang T, Zhang Z, Wallace OB, Deshpande M, Fang H, Yang Z, Zadjura LM, Tweedie DL, Huang S, Zhao F, Ranadive S, Robinson BS, Gong YF, Ricarrdi K, Spicer TP, Deminie C, Rose R, Wang HG, Blair WS, Shi PY, Lin PF, Colonno RJ, Meanwell NA. Wang T, et al. Among authors: lin pf. J Med Chem. 2003 Sep 25;46(20):4236-9. doi: 10.1021/jm034082o. J Med Chem. 2003. PMID: 13678401
Envelope conformational changes induced by human immunodeficiency virus type 1 attachment inhibitors prevent CD4 binding and downstream entry events.
Ho HT, Fan L, Nowicka-Sans B, McAuliffe B, Li CB, Yamanaka G, Zhou N, Fang H, Dicker I, Dalterio R, Gong YF, Wang T, Yin Z, Ueda Y, Matiskella J, Kadow J, Clapham P, Robinson J, Colonno R, Lin PF. Ho HT, et al. Among authors: lin pf. J Virol. 2006 Apr;80(8):4017-25. doi: 10.1128/JVI.80.8.4017-4025.2006. J Virol. 2006. PMID: 16571818 Free PMC article.
Inhibitors of HIV-1 attachment. Part 2: An initial survey of indole substitution patterns.
Meanwell NA, Wallace OB, Fang H, Wang H, Deshpande M, Wang T, Yin Z, Zhang Z, Pearce BC, James J, Yeung KS, Qiu Z, Kim Wright JJ, Yang Z, Zadjura L, Tweedie DL, Yeola S, Zhao F, Ranadive S, Robinson BA, Gong YF, Wang HG, Spicer TP, Blair WS, Shi PY, Colonno RJ, Lin PF. Meanwell NA, et al. Among authors: lin pf. Bioorg Med Chem Lett. 2009 Apr 1;19(7):1977-81. doi: 10.1016/j.bmcl.2009.02.040. Epub 2009 Feb 13. Bioorg Med Chem Lett. 2009. PMID: 19251416
Inhibitors of HIV-1 attachment. Part 3: A preliminary survey of the effect of structural variation of the benzamide moiety on antiviral activity.
Meanwell NA, Wallace OB, Wang H, Deshpande M, Pearce BC, Trehan A, Yeung KS, Qiu Z, Wright JJ, Robinson BA, Gong YF, Wang HG, Spicer TP, Blair WS, Shi PY, Lin PF. Meanwell NA, et al. Among authors: lin pf. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5136-9. doi: 10.1016/j.bmcl.2009.07.027. Epub 2009 Jul 10. Bioorg Med Chem Lett. 2009. PMID: 19632112
Inhibitors of HIV-1 attachment. Part 4: A study of the effect of piperazine substitution patterns on antiviral potency in the context of indole-based derivatives.
Wang T, Kadow JF, Zhang Z, Yin Z, Gao Q, Wu D, Parker DD, Yang Z, Zadjura L, Robinson BA, Gong YF, Spicer TP, Blair WS, Shi PY, Yamanaka G, Lin PF, Meanwell NA. Wang T, et al. Among authors: lin pf. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5140-5. doi: 10.1016/j.bmcl.2009.07.076. Epub 2009 Jul 18. Bioorg Med Chem Lett. 2009. PMID: 19664921
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. Among authors: lin pf. 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.
125 results