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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: yamanaka ga. J Med Chem. 2009 Dec 10;52(23):7778-87. doi: 10.1021/jm900843g. J Med Chem. 2009. PMID: 19769332
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. Among authors: yamanaka g. 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.
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: yamanaka g. 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.
161 results