Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 7, 2010, Pages 2264-2269

  Ma, Bin ^a   Guckian, Kevin M ^a   Lin, Edward Yin Shiang ^a   Lee, Wen Cherng ^a   Scott, Daniel ^a   Kumaravel, Gnanasambandam ^a   Macdonald, Timothy L ^b   Lynch, Kevin R ^c   Black, Cheryl ^a   Chollate, Sowmya ^a   Hahm, Kyungmin ^a   Hetu, Gregg ^a   Jin, Ping ^a   Luo, Yi ^a   Rohde, Ellen ^a   Rossomando, Anthony ^a   Scannevin, Robert ^a   Wang, Joy ^a   Yang, Chunhua ^a  

^a BIOGEN   (United States)

^b UNIVERSITY OF VIRGINIA   (United States)

^c UNIVERSITY OF VIRGINIA   (United States)

Author keywords

FTY720; Multiple sclerosis; Prodrug; S1P; SphK2; Tetralin; X ray

Indexed keywords

2 AMINO 2 ((S) 6 OCTYL 1,2,3,4 TETRAHYDRONAPHTHALEN 2 YL)PROPAN 1 OL; FINGOLIMOD; PRODRUG; SPHINGOSINE 1 PHOSPHATE 1 RECEPTOR AGONIST; SPHINGOSINE KINASE 2; TETRALIN DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; BIOAVAILABILITY; ENZYME SUBSTRATE; MOLECULAR PROBE; PHOSPHORYLATION; STEREOCHEMISTRY;

ADMINISTRATION, ORAL; ANIMALS; CRYSTALLOGRAPHY, X-RAY; IMMUNOSUPPRESSIVE AGENTS; LYMPHOPENIA; MICE; MODELS, MOLECULAR; MULTIPLE SCLEROSIS; PHOSPHORYLATION; PHOSPHOTRANSFERASES (ALCOHOL GROUP ACCEPTOR); PRODRUGS; RECEPTORS, LYSOSPHINGOLIPID; STRUCTURE-ACTIVITY RELATIONSHIP; TETRAHYDRONAPHTHALENES;

EID: 77949491449     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.02.006     Document Type: Article

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20. 3) δ 158.8, 135.89, 135.87, 133.40, 130.7, 129.37, 129.28, 126.2, 123.6, 74.4, 60.0, 43.5, 33.0, 31.7, 30.0, 29.5, 29.4, 28.9, 24.1, 23.4, 22.6, 14.1. LC-MS: m/z = 342.20 ([M+1], 100%).