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

2005; Elsevier BV; Volume: 15; Issue: 20 Linguagem: Inglês

10.1016/j.bmcl.2005.06.093

1464-3405

Jon J. Hangeland, Todd J. Friends, Arthur M. Doweyko, Karin Mellström, Johnny Sandberg, Marlena Grynfarb, Denis E. Ryono,

Chemical Synthesis and Analysis

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 TRbeta receptor and low to modest selectivity for TRbeta. They also exhibit an SAR that diverges from other thyromimetics that are based on the diaryl ether core found in 3,5,3'-triiodothyronine.