Discovery of Potent 3,5-Diphenyl-1,2,4-oxadiazole Sphingosine-1-phosphate-1 (S1P1) Receptor Agonists with Exceptional Selectivity against S1P2and S1P3

Zhen Li; Weirong Chen; Jeffrey J. Hale; Christopher L. Lynch; Sander G. Mills; Richard Hajdu; Carol Ann Keohane; Mark J. Rosenbach; James A. Milligan; Gan-Ju Shei; Gary Chrebet; Stephen A. Parent; James Bergstrom; Deborah Card; Michael Forrest; Elizabeth J. Quackenbush; L. Alexandra Wickham; Hugo Vargas; Rose M. Evans; Hugh Rosen; Suzanne Mandala

doi:10.1021/jm0503244

Discovery of Potent 3,5-Diphenyl-1,2,4-oxadiazole Sphingosine-1-phosphate-1 (S1P1) Receptor Agonists with Exceptional Selectivity against S1P2and S1P3

Journal of Medicinal Chemistry ◽

10.1021/jm0503244 ◽

2005 ◽

Vol 48 (20) ◽

pp. 6169-6173 ◽

Cited By ~ 69

Author(s):

Zhen Li ◽

Weirong Chen ◽

Jeffrey J. Hale ◽

Christopher L. Lynch ◽

Sander G. Mills ◽

...

Keyword(s):

Receptor Agonists ◽

S1p1 Receptor ◽

Sphingosine 1 Phosphate

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Indole-propionic acid derivatives as potent, S1P3-sparing and EAE efficacious sphingosine-1-phosphate 1 (S1P1) receptor agonists

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2012.02.083 ◽

2012 ◽

Vol 22 (8) ◽

pp. 2794-2797 ◽

Cited By ~ 9

Author(s):

Qinghua Meng ◽

Baowei Zhao ◽

Qiongfeng Xu ◽

Xuesong Xu ◽

Guanghui Deng ◽

...

Keyword(s):

Propionic Acid ◽

Receptor Agonists ◽

S1p1 Receptor ◽

Sphingosine 1 Phosphate

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

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2005.05.097 ◽

2005 ◽

Vol 15 (15) ◽

pp. 3568-3572 ◽

Cited By ~ 27

Author(s):

Jeremy J. Clemens ◽

Michael D. Davis ◽

Kevin R. Lynch ◽

Timothy L. Macdonald

Keyword(s):

Receptor Agonists ◽

S1p1 Receptor ◽

Sphingosine 1 Phosphate

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Pyrazole derived from (+)-3-carene; a novel potent, selective scaffold for sphingosine-1-phosphate (S1P1) receptor agonists

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2009.11.045 ◽

2010 ◽

Vol 20 (1) ◽

pp. 35-37 ◽

Cited By ~ 5

Author(s):

Frédéric J. Zécri ◽

Rainer Albert ◽

Gregory Landrum ◽

Klaus Hinterding ◽

Nigel G. Cooke ◽

...

Keyword(s):

Receptor Agonists ◽

S1p1 Receptor ◽

Sphingosine 1 Phosphate

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Faculty Opinions recommendation of Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1064759.517678 ◽

2007 ◽

Author(s):

Hugh Rosen

Keyword(s):

Biological Evaluation ◽

Receptor Agonists ◽

Sphingosine 1 Phosphate ◽

Subtype Selective ◽

Synthesis And Biological Evaluation ◽

Receptor Agonists And Antagonists

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Design, synthesis and docking-based 3D-QSAR study of novel 2-substituted 2-aminopropane-1,3-diols as potent and selective agonists of sphingosine-1-phosphate 1 (S1P1) receptor

MedChemComm ◽

10.1039/c3md00079f ◽

2013 ◽

Vol 4 (9) ◽

pp. 1267 ◽

Cited By ~ 16

Author(s):

Yulin Tian ◽

Jing Jin ◽

Xiaojian Wang ◽

Weijuan Han ◽

Gang Li ◽

...

Keyword(s):

3D Qsar ◽

Qsar Study ◽

Design Synthesis ◽

S1p1 Receptor ◽

Sphingosine 1 Phosphate ◽

Selective Agonists

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Immune Cell Regulation and Cardiovascular Effects of Sphingosine 1-Phosphate Receptor Agonists in Rodents Are Mediated via Distinct Receptor Subtypes

Journal of Pharmacology and Experimental Therapeutics ◽

10.1124/jpet.103.062828 ◽

2004 ◽

Vol 309 (2) ◽

pp. 758-768 ◽

Cited By ~ 253

Author(s):

M. Forrest ◽

S.-Y. Sun ◽

R. Hajdu ◽

J. Bergstrom ◽

D. Card ◽

...

Keyword(s):

Immune Cell ◽

Cardiovascular Effects ◽

Receptor Subtypes ◽

Cell Regulation ◽

Receptor Agonists ◽

Sphingosine 1 Phosphate

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Sphingosine‐1‐Phosphate‐Mediated Endothelial Cell Motility Is Regulated by S1P1 Receptor, Lipid Phosphate Phosphatase‐1 and Sphingosine Kinase 1

The FASEB Journal ◽

10.1096/fasebj.20.4.a483-a ◽

2006 ◽

Vol 20 (4) ◽

Author(s):

Irina Gorshkova ◽

Evgeny Berdyshev ◽

Bahman Saatian ◽

Yutong Zhao ◽

Srikanth Pendyala ◽

...

Keyword(s):

Endothelial Cell ◽

Cell Motility ◽

Sphingosine Kinase ◽

Sphingosine Kinase 1 ◽

S1p1 Receptor ◽

Sphingosine 1 Phosphate ◽

Lipid Phosphate

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Alignment independent 3D-QSAR studies and molecular dynamics simulations for the identification of potent and selective S1P1 receptor agonists

Journal of Molecular Graphics and Modelling ◽

10.1016/j.jmgm.2019.107459 ◽

2020 ◽

Vol 94 ◽

pp. 107459

Author(s):

Ali Akbar Alizadeh ◽

Behzad Jafari ◽

Siavoush Dastmalchi

Keyword(s):

Molecular Dynamics ◽

Molecular Dynamics Simulations ◽

3D Qsar ◽

Qsar Studies ◽

Receptor Agonists ◽

S1p1 Receptor ◽

Dynamics Simulations

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39 REGULATION OF SPHINGOSINE 1-PHOSPHATE-INDUCED ENDOTHELIAL CYTOSKELETAL REARRANGEMENT AND BARRIER ENHANCEMENT BY S1P1 RECEPTOR, CAVEOLIN-ENRICHED MICRODOMAINS, PI3 KINASE AND TIAM1/RAC1

Journal of Investigative Medicine ◽

10.2310/6650.2005.00206.38 ◽

2005 ◽

Vol 53 (2) ◽

pp. S363.3-S363

Author(s):

P. A. Singleton ◽

J. G.N. Garcia

Keyword(s):

Pi3 Kinase ◽

S1p1 Receptor ◽

Cytoskeletal Rearrangement ◽

Sphingosine 1 Phosphate

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Novel S1P1 receptor agonists – Part 5: From amino-to alkoxy-pyridines

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2016.03.020 ◽

2016 ◽

Vol 115 ◽

pp. 326-341 ◽

Cited By ~ 6

Author(s):

Martin H. Bolli ◽

Cyrille Lescop ◽

Magdalena Birker ◽

Ruben de Kanter ◽

Patrick Hess ◽

...

Keyword(s):

Receptor Agonists ◽

S1p1 Receptor

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