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Discovery of potent 3,5-diphenyl-1,2,4-oxadiazole sphingosine-1-phosphate-1 (S1P1) receptor agonists with exceptional selectivity against S1P2 and S1P3.
Li Z, Chen W, Hale JJ, Lynch CL, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Chrebet G, Parent SA, Bergstrom J, Card D, Forrest M, Quackenbush EJ, Wickham LA, Vargas H, Evans RM, Rosen H, Mandala S. Li Z, et al. Among authors: mandala s. J Med Chem. 2005 Oct 6;48(20):6169-73. doi: 10.1021/jm0503244. J Med Chem. 2005. PMID: 16190743
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. 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
Discovery of 3-arylpropionic acids as potent agonists of sphingosine-1-phosphate receptor-1 (S1P1) with high selectivity against all other known S1P receptor subtypes.
Yan L, Huo P, Doherty G, Toth L, Hale JJ, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Chrebet G, Bergstrom J, Card D, Quackenbush E, Wickham A, Mandala SM. Yan L, et al. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3679-83. doi: 10.1016/j.bmcl.2006.04.084. Epub 2006 May 11. Bioorg Med Chem Lett. 2006. PMID: 16697189
Alteration of lymphocyte trafficking by sphingosine-1-phosphate receptor agonists.
Mandala S, Hajdu R, Bergstrom J, Quackenbush E, Xie J, Milligan J, Thornton R, Shei GJ, Card D, Keohane C, Rosenbach M, Hale J, Lynch CL, Rupprecht K, Parsons W, Rosen H. Mandala S, et al. Science. 2002 Apr 12;296(5566):346-9. doi: 10.1126/science.1070238. Epub 2002 Mar 28. Science. 2002. PMID: 11923495
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: mandala s. 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: mandala s. 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
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