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Page 1
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: malkowitz l. J Nat Prod. 2004 Jun;67(6):1036-8. doi: 10.1021/np049974l. J Nat Prod. 2004. PMID: 15217290
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: malkowitz l. 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: malkowitz l. 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
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: malkowitz l. 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
Combinatorial synthesis of CCR5 antagonists.
Willoughby CA, Berk SC, Rosauer KG, Degrado S, Chapman KT, Gould SL, Springer MS, Malkowitz L, Schleif WA, Hazuda D, Miller M, Kessler J, Danzeisen R, Holmes K, Lineberger J, Carella A, Carver G, Emini EA. Willoughby CA, et al. Among authors: malkowitz l. Bioorg Med Chem Lett. 2001 Dec 17;11(24):3137-41. doi: 10.1016/s0960-894x(01)00652-7. Bioorg Med Chem Lett. 2001. PMID: 11720860
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: malkowitz l. 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.
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 3: a proposed pharmacophore model for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-[4-(substituted)piperidin-1-yl]butanes.
Finke PE, Meurer LC, Oates B, Shah SK, Loebach JL, Mills SG, MacCoss M, Castonguay L, Malkowitz L, Springer MS, Gould SL, DeMartino JA. Finke PE, et al. Among authors: malkowitz l. Bioorg Med Chem Lett. 2001 Sep 17;11(18):2469-73. doi: 10.1016/s0960-894x(01)00491-7. Bioorg Med Chem Lett. 2001. PMID: 11549449
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: synthesis and structure-activity relationships for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes.
Finke PE, Oates B, Mills SG, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, 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: malkowitz l. Bioorg Med Chem Lett. 2001 Sep 17;11(18):2475-9. doi: 10.1016/s0960-894x(01)00492-9. Bioorg Med Chem Lett. 2001. PMID: 11549450
Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection.
Kim D, Wang L, Caldwell CG, Chen P, Finke PE, Oates B, MacCoss M, Mills SG, Malkowitz L, Gould SL, DeMartino JA, Springer MS, Hazuda D, Miller M, Kessler J, Danzeisen R, Carver G, Carella A, Holmes K, Lineberger J, Schleif WA, Emini EA. Kim D, et al. Among authors: malkowitz l. Bioorg Med Chem Lett. 2001 Dec 17;11(24):3099-102. doi: 10.1016/s0960-894x(01)00654-0. Bioorg Med Chem Lett. 2001. PMID: 11720851
37 results