A new class of high affinity thyromimetics containing a phenyl-naphthylene core

High affinity thyromimetics containing a novel phenyl-naphthylene core are reported. The functionalized core is readily accessible via a Suzuki coupling protocol. Examples of this new class of TR ligands have sub-nanomolar binding affinities for the TRβ receptor and low to modest selectivity for TRβ. They also exhibit an SAR that diverges from other thyromimetics that are based on the diaryl ether core found in 3,5,3′-triiodothyronine.

Graphical abstractExamples of this new class of thyromimetics have sub-nanomolar binding affinities for TR, with an SAR that diverges from TR ligands containing a biaryl ether core.Figure optionsDownload full-size imageDownload as PowerPoint slide