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Results: 1 to 20 of 107

1.

Novel S1P1 receptor agonists--part 1: From pyrazoles to thiophenes.

Bolli MH, Müller C, Mathys B, Abele S, Birker M, Bravo R, Bur D, Hess P, Kohl C, Lehmann D, Nayler O, Rey M, Meyer S, Scherz M, Schmidt G, Steiner B, Treiber A, Velker J, Weller T.

J Med Chem. 2013 Dec 12;56(23):9737-55. doi: 10.1021/jm4014373. Epub 2013 Nov 22.

PMID:
24266709
[PubMed - indexed for MEDLINE]
2.

Novel S1P(1) receptor agonists--part 3: from thiophenes to pyridines.

Bolli MH, Abele S, Birker M, Bravo R, Bur D, de Kanter R, Kohl C, Grimont J, Hess P, Lescop C, Mathys B, Müller C, Nayler O, Rey M, Scherz M, Schmidt G, Seifert J, Steiner B, Velker J, Weller T.

J Med Chem. 2014 Jan 9;57(1):110-30. doi: 10.1021/jm4014696. Epub 2013 Dec 24.

PMID:
24367923
[PubMed - indexed for MEDLINE]
3.

Novel S1P(1) receptor agonists--part 2: from bicyclo[3.1.0]hexane-fused thiophenes to isobutyl substituted thiophenes.

Bolli MH, Velker J, Müller C, Mathys B, Birker M, Bravo R, Bur D, de Kanter R, Hess P, Kohl C, Lehmann D, Meyer S, Nayler O, Rey M, Scherz M, Steiner B.

J Med Chem. 2014 Jan 9;57(1):78-97. doi: 10.1021/jm401456d. Epub 2013 Dec 17.

PMID:
24345087
[PubMed - indexed for MEDLINE]
4.

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.

J Med Chem. 2005 Oct 6;48(20):6169-73.

PMID:
16190743
[PubMed - indexed for MEDLINE]
5.

Highly selective and potent agonists of sphingosine-1-phosphate 1 (S1P1) receptor.

Vachal P, Toth LM, Hale JJ, Yan L, Mills SG, Chrebet GL, Koehane CA, Hajdu R, Milligan JA, Rosenbach MJ, Mandala S.

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3684-7. Epub 2006 May 6.

PMID:
16682185
[PubMed - indexed for MEDLINE]
6.

Protective effects of sphingosine-1-phosphate receptor agonist treatment after myocardial ischaemia-reperfusion.

Hofmann U, Burkard N, Vogt C, Thoma A, Frantz S, Ertl G, Ritter O, Bonz A.

Cardiovasc Res. 2009 Jul 15;83(2):285-93. doi: 10.1093/cvr/cvp137. Epub 2009 May 5.

PMID:
19416991
[PubMed - indexed for MEDLINE]
Free Article
7.

Identification of Leu276 of the S1P1 receptor and Phe263 of the S1P3 receptor in interaction with receptor specific agonists by molecular modeling, site-directed mutagenesis, and affinity studies.

Deng Q, Clemas JA, Chrebet G, Fischer P, Hale JJ, Li Z, Mills SG, Bergstrom J, Mandala S, Mosley R, Parent SA.

Mol Pharmacol. 2007 Mar;71(3):724-35. Epub 2006 Dec 14.

PMID:
17170199
[PubMed - indexed for MEDLINE]
Free Article
8.

Discovery of a novel series of potent S1P1 agonists.

Crosignani S, Bombrun A, Covini D, Maio M, Marin D, Quattropani A, Swinnen D, Simpson D, Sauer W, Françon B, Martin T, Cambet Y, Nichols A, Martinou I, Burgat-Charvillon F, Rivron D, Donini C, Schott O, Eligert V, Novo-Perez L, Vitte PA, Arrighi JF.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1516-9. doi: 10.1016/j.bmcl.2010.01.102. Epub 2010 Jan 25.

PMID:
20149651
[PubMed - indexed for MEDLINE]
9.

Discovery of CS-2100, a potent, orally active and S1P3-sparing S1P1 agonist.

Nakamura T, Asano M, Sekiguchi Y, Mizuno Y, Tamaki K, Kimura T, Nara F, Kawase Y, Shimozato T, Doi H, Kagari T, Tomisato W, Inoue R, Nagasaki M, Yuita H, Oguchi-Oshima K, Kaneko R, Watanabe N, Abe Y, Nishi T.

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1788-92. doi: 10.1016/j.bmcl.2011.12.019. Epub 2012 Jan 2.

PMID:
22264485
[PubMed - indexed for MEDLINE]
10.

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.

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3679-83. Epub 2006 May 11.

PMID:
16697189
[PubMed - indexed for MEDLINE]
11.

Ligand-binding pocket shape differences between sphingosine 1-phosphate (S1P) receptors S1P1 and S1P3 determine efficiency of chemical probe identification by ultrahigh-throughput screening.

Schürer SC, Brown SJ, Gonzalez-Cabrera PJ, Schaeffer MT, Chapman J, Jo E, Chase P, Spicer T, Hodder P, Rosen H.

ACS Chem Biol. 2008 Aug 15;3(8):486-98. doi: 10.1021/cb800051m. Epub 2008 Jul 1.

PMID:
18590333
[PubMed - indexed for MEDLINE]
Free PMC Article
12.

Pyrazole derived from (+)-3-carene; a novel potent, selective scaffold for sphingosine-1-phosphate (S1P(1)) receptor agonists.

Zécri FJ, Albert R, Landrum G, Hinterding K, Cooke NG, Guerini D, Streiff M, Bruns C, Nuesslein-Hildesheim B.

Bioorg Med Chem Lett. 2010 Jan 1;20(1):35-7. doi: 10.1016/j.bmcl.2009.11.045. Epub 2009 Nov 15.

PMID:
19954976
[PubMed - indexed for MEDLINE]
13.

2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.

Bolli MH, Abele S, Binkert C, Bravo R, Buchmann S, Bur D, Gatfield J, Hess P, Kohl C, Mangold C, Mathys B, Menyhart K, Müller C, Nayler O, Scherz M, Schmidt G, Sippel V, Steiner B, Strasser D, Treiber A, Weller T.

J Med Chem. 2010 May 27;53(10):4198-211. doi: 10.1021/jm100181s.

PMID:
20446681
[PubMed - indexed for MEDLINE]
14.

Discovery and structural optimization of pyrazole derivatives as novel inhibitors of Cdc25B.

Chen HJ, Liu Y, Wang LN, Shen Q, Li J, Nan FJ.

Bioorg Med Chem Lett. 2010 May 1;20(9):2876-9. doi: 10.1016/j.bmcl.2010.03.040. Epub 2010 Mar 11.

PMID:
20363629
[PubMed - indexed for MEDLINE]
15.

Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P₃-sparing S1P₁ agonists.

Asano M, Nakamura T, Sekiguchi Y, Mizuno Y, Yamaguchi T, Tamaki K, Shimozato T, Doi-Komuro H, Kagari T, Tomisato W, Inoue R, Yuita H, Oguchi-Oshima K, Kaneko R, Nara F, Kawase Y, Masubuchi N, Nakayama S, Koga T, Namba E, Nasu H, Nishi T.

Bioorg Med Chem Lett. 2012 May 1;22(9):3083-8. doi: 10.1016/j.bmcl.2012.03.067. Epub 2012 Mar 23.

PMID:
22487179
[PubMed - indexed for MEDLINE]
16.

A novel sphingosine-1-phosphate receptor 1 antagonist prevents the proliferation and relaxation of vascular endothelial cells by sphingosine-1-phosphate.

Yonesu K, Nakamura T, Mizuno Y, Suzuki C, Nagayama T, Satoh S, Nara F.

Biol Pharm Bull. 2010;33(9):1500-5.

PMID:
20823564
[PubMed - indexed for MEDLINE]
Free Article
17.

Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.

Clemens JJ, Davis MD, Lynch KR, Macdonald TL.

Bioorg Med Chem Lett. 2005 Aug 1;15(15):3568-72.

PMID:
15982878
[PubMed - indexed for MEDLINE]
18.

New players on the center stage: sphingosine 1-phosphate and its receptors as drug targets.

Huwiler A, Pfeilschifter J.

Biochem Pharmacol. 2008 May 15;75(10):1893-900. doi: 10.1016/j.bcp.2007.12.018. Epub 2008 Jan 5. Review.

PMID:
18321471
[PubMed - indexed for MEDLINE]
19.

Ligand-dependent inhibition of B16 melanoma cell migration and invasion via endogenous S1P2 G protein-coupled receptor. Requirement of inhibition of cellular RAC activity.

Arikawa K, Takuwa N, Yamaguchi H, Sugimoto N, Kitayama J, Nagawa H, Takehara K, Takuwa Y.

J Biol Chem. 2003 Aug 29;278(35):32841-51. Epub 2003 Jun 16.

PMID:
12810709
[PubMed - indexed for MEDLINE]
Free Article
20.

Selective sphingosine 1-phosphate 1 receptor activation reduces ischemia-reperfusion injury in mouse kidney.

Awad AS, Ye H, Huang L, Li L, Foss FW Jr, Macdonald TL, Lynch KR, Okusa MD.

Am J Physiol Renal Physiol. 2006 Jun;290(6):F1516-24. Epub 2006 Jan 10.

PMID:
16403835
[PubMed - indexed for MEDLINE]
Free Article

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