Literature

Abstract

Fluorescently labeled chiral analogs of the immunomodulatory drug FTY720 and its corresponding phosphates with variable aliphatic spacers between the aromatic ring and the NBD label have been synthesized. Determining the influence of the spacer on the in vitro phosphorylation rate by SPHK1 and 2 resulted in the identification of NBD-(R)-AAL 1c,d which are phosphorylated with an efficiency comparable to that of the unlabeled FTY720 analog (R)-AAL. Furthermore, the NBD-(R)-AAL phosphates 10c,d were proven to be a functional S1P receptor agonist.

DOI： 10.1016/j.bmcl.2005.09.038

NBD-labeled derivatives of the immunomodulatory drug FTY720 as tools for metabolism and mode of action studies

Bioorganic & Medicinal Chemistry Letters 2006.0

Constrained azacyclic analogues of the immunomodulatory agent FTY720 as molecular probes for sphingosine 1-phosphate receptors

Bioorganic & Medicinal Chemistry Letters 2007.0

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

Bioorganic & Medicinal Chemistry Letters 2005.0

Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720

Bioorganic & Medicinal Chemistry Letters 2004.0

New fluorinated agonists for targeting the sphingosin-1-phosphate receptor 1 (S1P1)

Bioorganic & Medicinal Chemistry Letters 2015.0

Synthesis and Evaluation of Fluorinated Fingolimod (FTY720) Analogues for Sphingosine-1-Phosphate Receptor Molecular Imaging by Positron Emission Tomography