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A new class of high affinity thyromimetics containing a phenyl-naphthylene core.
Hangeland, Jon J; Friends, Todd J; Doweyko, Arthur M; Mellström, Karin; Sandberg, Johnny; Grynfarb, Marlena; Ryono, Denis E.
Affiliation
  • Hangeland JJ; Pharmaceutical Research Institute, Bristol-Myers Squibb, Princeton, NJ 08543-5400, USA. jon.hangeland@bms.com
Bioorg Med Chem Lett ; 15(20): 4579-84, 2005 Oct 15.
Article in En | MEDLINE | ID: mdl-16099653
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 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.
Subject(s)
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Collection: 01-internacional Database: MEDLINE Main subject: Thyroid Hormones / Receptors, Thyroid Hormone / Naphthalenes Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2005 Document type: Article Affiliation country: United States
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Collection: 01-internacional Database: MEDLINE Main subject: Thyroid Hormones / Receptors, Thyroid Hormone / Naphthalenes Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2005 Document type: Article Affiliation country: United States
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