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Page 1
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: mills sg. 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
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: mills sg. 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: mills sg. 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
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: mills sg. 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: mills sg. 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
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: mills sg. 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
Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor 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: mills sg. Bioorg Med Chem Lett. 2001 Dec 17;11(24):3103-6. doi: 10.1016/s0960-894x(01)00655-2. Bioorg Med Chem Lett. 2001. PMID: 11720852
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
Hale JJ, Mills SG, MacCoss M, Finke PE, Cascieri MA, Sadowski S, Ber E, Chicchi GG, Kurtz M, Metzger J, Eiermann G, Tsou NN, Tattersall FD, Rupniak NM, Williams AR, Rycroft W, Hargreaves R, MacIntyre DE. Hale JJ, et al. Among authors: mills sg. J Med Chem. 1998 Nov 5;41(23):4607-14. doi: 10.1021/jm980299k. J Med Chem. 1998. PMID: 9804700
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
Hale JJ, Mills SG, MacCoss M, Dorn CP, Finke PE, Budhu RJ, Reamer RA, Huskey SE, Luffer-Atlas D, Dean BJ, McGowan EM, Feeney WP, Chiu SH, Cascieri MA, Chicchi GG, Kurtz MM, Sadowski S, Ber E, Tattersall FD, Rupniak NM, Williams AR, Rycroft W, Hargreaves R, Metzger JM, MacIntyre DE. Hale JJ, et al. Among authors: mills sg. J Med Chem. 2000 Mar 23;43(6):1234-41. doi: 10.1021/jm990617v. J Med Chem. 2000. PMID: 10737756
87 results