Synthesis, stability, and implications of phosphothioate agonists of sphingosine-1-phosphate receptors
Graphical abstract
The synthesis and biological activity of phosphothioates, as subtype selective sphingosine-1-phosphate receptor agonists, are described. Sphingosine-1-phosphate receptor agonist 12 is degraded to its alcohol in vivo. Compared to their phosphate precursors, phosphothioate compounds 7 and 13 were shown to induce lymphopenia for protracted intervals in vivo.
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Acknowledgments
This work was supported by grants from the NIH [NIGMS R01 GM067958 (to K.R.L.) and NIGMS F31 GM064101 (to M.D.D.)].
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