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

…, K Mellström, J Sandberg, M Grynfarb…

文献索引: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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被引用次数: 11

摘要

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.