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

…, K Mellström, J Sandberg, M Grynfarb…

Index: Hangeland, Jon J.; Friends, Todd J.; Doweyko, Arthur M.; Mellstroem, Karin; Sandberg, Johnny; Grynfarb, Marlena; Ryono, Denis E. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 20 p. 4579 - 4584

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Citation Number: 11

Abstract

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.