Abstract
transTetrafluoro-λ6-sulfane (tetrafluorosulfanyl, SF4) compounds possess unique properties, including a linear structure and high electronegativity. Here, to investigate the utility of the trans-SF4 moiety as a structural element of bioactive compounds, we designed and synthesized novel retinoids containing a trans-SF4-alkynyl group as a linear linker. The radical addition reaction of aryltetrafluorosulfanyl chloride and arylethyne, followed by elimination of hydrogen chloride, afforded the target compounds 1a – 1c. Cell differentiation-inducing activity assay and reporter gene assay revealed that the trans-SF4-alkynyl derivatives 1b and 1c exhibit antagonistic activity towards retinoid acid receptors (RARs). Docking studies suggested that the long and linear linker alters the binding mode of 1b with the RARα ligand-binding domain.
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