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1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity.
Hale JJ, Budhu RJ, Holson EB, Finke PE, Oates B, Mills SG, MacCoss M, Gould SL, DeMartino JA, Springer MS, Siciliano S, Malkowitz L, Schleif WA, Hazuda D, Miller M, Kessler J, Danzeisen R, Holmes K, Lineberger J, Carella A, Carver G, Emini E. Hale JJ, et al. Among authors: siciliano s. Bioorg Med Chem Lett. 2001 Oct 22;11(20):2741-5. doi: 10.1016/s0960-894x(01)00545-5. Bioorg Med Chem Lett. 2001. PMID: 11591514
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. part 1: discovery and initial structure-activity relationships for 1 -amino-2-phenyl-4-(piperidin-1-yl)butanes.
Dorn CP, Finke PE, Oates B, Budhu RJ, Mills SG, MacCoss M, Malkowitz L, Springer MS, Daugherty BL, Gould SL, DeMartino JA, Siciliano SJ, Carella A, Carver G, Holmes K, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Schleif WA, Emini EA. Dorn CP, et al. Among authors: siciliano sj. Bioorg Med Chem Lett. 2001 Jan 22;11(2):259-64. doi: 10.1016/s0960-894x(00)00637-5. Bioorg Med Chem Lett. 2001. PMID: 11206473
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: structure-activity relationships for substituted 2-Aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes.
Finke PE, Meurer LC, Oates B, Mills SG, MacCoss M, Malkowitz L, Springer MS, Daugherty BL, Gould SL, DeMartino JA, Siciliano SJ, Carella A, Carver G, Holmes K, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Schleif WA, Emini EA. Finke PE, et al. Among authors: siciliano sj. Bioorg Med Chem Lett. 2001 Jan 22;11(2):265-70. doi: 10.1016/s0960-894x(00)00639-9. Bioorg Med Chem Lett. 2001. PMID: 11206474
Isolation and structure of antagonists of chemokine receptor (CCR5).
Jayasuriya H, Herath KB, Ondeyka JG, Polishook JD, Bills GF, Dombrowski AW, Springer MS, Siciliano S, Malkowitz L, Sanchez M, Guan Z, Tiwari S, Stevenson DW, Borris RP, Singh SB. Jayasuriya H, et al. Among authors: siciliano s. J Nat Prod. 2004 Jun;67(6):1036-8. doi: 10.1021/np049974l. J Nat Prod. 2004. PMID: 15217290
CCR5, CXCR4, and CD4 are clustered and closely apposed on microvilli of human macrophages and T cells.
Singer II, Scott S, Kawka DW, Chin J, Daugherty BL, DeMartino JA, DiSalvo J, Gould SL, Lineberger JE, Malkowitz L, Miller MD, Mitnaul L, Siciliano SJ, Staruch MJ, Williams HR, Zweerink HJ, Springer MS. Singer II, et al. Among authors: siciliano sj. J Virol. 2001 Apr;75(8):3779-90. doi: 10.1128/JVI.75.8.3779-3790.2001. J Virol. 2001. PMID: 11264367 Free PMC article.
Substituted 4,6-diaminoquinolines as inhibitors of C5a receptor binding.
Lanza TJ, Durette PL, Rollins T, Siciliano S, Cianciarulo DN, Kobayashi SV, Caldwell CG, Springer MS, Hagmann WK. Lanza TJ, et al. Among authors: siciliano s. J Med Chem. 1992 Jan 24;35(2):252-8. doi: 10.1021/jm00080a008. J Med Chem. 1992. PMID: 1310118
328 results