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Page 1
Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors.
Yan L, Hale JJ, Lynch CL, Budhu R, Gentry A, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Chrebet G, Bergstrom J, Card D, Rosen H, Mandala SM. Yan L, et al. Among authors: mills sg. Bioorg Med Chem Lett. 2004 Oct 4;14(19):4861-6. doi: 10.1016/j.bmcl.2004.07.049. Bioorg Med Chem Lett. 2004. PMID: 15341940
Immune cell regulation and cardiovascular effects of sphingosine 1-phosphate receptor agonists in rodents are mediated via distinct receptor subtypes.
Forrest M, Sun SY, Hajdu R, Bergstrom J, Card D, Doherty G, Hale J, Keohane C, Meyers C, Milligan J, Mills S, Nomura N, Rosen H, Rosenbach M, Shei GJ, Singer II, Tian M, West S, White V, Xie J, Proia RL, Mandala S. Forrest M, et al. J Pharmacol Exp Ther. 2004 May;309(2):758-68. doi: 10.1124/jpet.103.062828. Epub 2004 Jan 27. J Pharmacol Exp Ther. 2004. PMID: 14747617
CCR5 antagonists: bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines.
Lynch CL, Gentry AL, Hale JJ, Mills SG, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Doss G, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA. Lynch CL, et al. Among authors: mills sg. Bioorg Med Chem Lett. 2002 Feb 25;12(4):677-9. doi: 10.1016/s0960-894x(01)00835-6. Bioorg Med Chem Lett. 2002. PMID: 11844699
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV.
Lynch CL, Hale JJ, Budhu RJ, Gentry AL, Mills SG, Chapman KT, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA. Lynch CL, et al. Among authors: mills sg. Bioorg Med Chem Lett. 2002 Oct 21;12(20):3001-4. doi: 10.1016/s0960-894x(02)00606-6. Bioorg Med Chem Lett. 2002. PMID: 12270193
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains.
Lynch CL, Willoughby CA, Hale JJ, Holson EJ, Budhu RJ, Gentry AL, Rosauer KG, Caldwell CG, Chen P, Mills SG, MacCoss M, Berk S, Chen L, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA. Lynch CL, et al. Among authors: mills sg. Bioorg Med Chem Lett. 2003 Jan 6;13(1):119-23. doi: 10.1016/s0960-894x(02)00829-6. Bioorg Med Chem Lett. 2003. PMID: 12467630
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds.
Shen DM, Shu M, Willoughby CA, Shah S, Lynch CL, Hale JJ, Mills SG, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Lyons K, Pivnichny JV, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA. Shen DM, et al. Among authors: mills sg. Bioorg Med Chem Lett. 2004 Feb 23;14(4):941-5. doi: 10.1016/j.bmcl.2003.12.005. Bioorg Med Chem Lett. 2004. PMID: 15012998
The discovery of 3-(N-alkyl)aminopropylphosphonic acids as potent S1P receptor agonists.
Hale JJ, Doherty G, Toth L, Li Z, Mills SG, Hajdu R, Ann Keohane C, Rosenbach M, Milligan J, Shei GJ, Chrebet G, Bergstrom J, Card D, Rosen H, Mandala S. Hale JJ, et al. Among authors: mills sg. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3495-9. doi: 10.1016/j.bmcl.2004.04.069. Bioorg Med Chem Lett. 2004. PMID: 15177460
Selecting against S1P3 enhances the acute cardiovascular tolerability of 3-(N-benzyl)aminopropylphosphonic acid S1P receptor agonists.
Hale JJ, Doherty G, Toth L, Mills SG, Hajdu R, Keohane CA, Rosenbach M, Milligan J, Shei GJ, Chrebet G, Bergstrom J, Card D, Forrest M, Sun SY, West S, Xie H, Nomura N, Rosen H, Mandala S. Hale JJ, et al. Among authors: mills sg. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3501-5. doi: 10.1016/j.bmcl.2004.04.070. Bioorg Med Chem Lett. 2004. PMID: 15177461
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.
Hale JJ, Lynch CL, Neway W, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Parent SA, Chrebet G, Bergstrom J, Card D, Ferrer M, Hodder P, Strulovici B, Rosen H, Mandala S. Hale JJ, et al. Among authors: mills sg. J Med Chem. 2004 Dec 30;47(27):6662-5. doi: 10.1021/jm0492507. J Med Chem. 2004. PMID: 15615513
84 results