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Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir.
Wang T, Ueda Y, Zhang Z, Yin Z, Matiskella J, Pearce BC, Yang Z, Zheng M, Parker DD, Yamanaka GA, Gong YF, Ho HT, Colonno RJ, Langley DR, Lin PF, Meanwell NA, Kadow JF. Wang T, et al. Among authors: yang z. J Med Chem. 2018 Jul 26;61(14):6308-6327. doi: 10.1021/acs.jmedchem.8b00759. Epub 2018 Jul 13. J Med Chem. 2018. PMID: 29920093
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: yang z. 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. 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. Among authors: yang z. J Med Chem. 2013 Feb 28;56(4):1656-69. doi: 10.1021/jm3016377. Epub 2013 Feb 7. J Med Chem. 2013. PMID: 23360431
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: yang z. J Med Chem. 2003 Sep 25;46(20):4236-9. doi: 10.1021/jm034082o. J Med Chem. 2003. PMID: 13678401
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: yang z. 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 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: yang z. 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
Inhibitors of HIV-1 attachment. Part 9: an assessment of oral prodrug approaches to improve the plasma exposure of a tetrazole-containing derivative.
Yeung KS, Qiu Z, Yang Z, Zadjura L, D'Arienzo CJ, Browning MR, Hansel S, Huang XS, Eggers BJ, Riccardi K, Lin PF, Meanwell NA, Kadow JF. Yeung KS, et al. Among authors: yang z. Bioorg Med Chem Lett. 2013 Jan 1;23(1):209-12. doi: 10.1016/j.bmcl.2012.10.125. Epub 2012 Nov 7. Bioorg Med Chem Lett. 2013. PMID: 23200244
Inhibitors of HIV-1 attachment. Part 8: the effect of C7-heteroaryl substitution on the potency, and in vitro and in vivo profiles of indole-based inhibitors.
Yeung KS, Qiu Z, Yin Z, Trehan A, Fang H, Pearce B, Yang Z, Zadjura L, D'Arienzo CJ, Riccardi K, Shi PY, Spicer TP, Gong YF, Browning MR, Hansel S, Santone K, Barker J, Coulter T, Lin PF, Meanwell NA, Kadow JF. Yeung KS, et al. Among authors: yang z. Bioorg Med Chem Lett. 2013 Jan 1;23(1):203-8. doi: 10.1016/j.bmcl.2012.10.117. Epub 2012 Nov 5. Bioorg Med Chem Lett. 2013. PMID: 23200249
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