Design, synthesis, and in vitro bioactivity evaluation of fluorine-containing analogues for sphingosine-1-phosphate 2 receptor

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Abstract

Twenty eight new aryloxybenzene analogues were synthesized and their in vitro binding potencies toward S1PR2 were determined using a [32P]S1P competitive binding assay. Out of these new analogues, three compounds, 28c (IC50 = 29.9 ± 3.9 nM), 28e (IC50 = 14.6 ± 1.5 nM), and 28g (IC50 = 38.5 ± 6.3 nM) exhibited high binding potency toward S1PR2 and high selectivity over the other four receptor subtypes (S1PR1, 3, 4, and 5; IC50 > 1000 nM). Each of the three potent compounds 28c, 28e, and 28g contains a fluorine atom that will allow to develop F-18 labeled PET radiotracers for imaging S1PR2.

Original languageEnglish
Pages (from-to)3619-3631
Number of pages13
JournalBioorganic and Medicinal Chemistry
Volume27
Issue number16
DOIs
StatePublished - Aug 15 2019

Keywords

  • Binding potency
  • Positron emission tomography
  • Selectivity
  • Sphingosine 1-phosphate receptor 2

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