A new class of high affinity thyromimetics containing a phenyl-naphthylene core.
Article Details
- CitationCopy to clipboard
Hangeland JJ, Friends TJ, Doweyko AM, Mellstrom K, Sandberg J, Grynfarb M, Ryono DE
A new class of high affinity thyromimetics containing a phenyl-naphthylene core.
Bioorg Med Chem Lett. 2005 Oct 15;15(20):4579-84.
- PubMed ID
- 16099653 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) KB-141 Thyroid hormone receptor alpha IC 50 (nM) 25 N/A N/A Details KB-141 Thyroid hormone receptor beta IC 50 (nM) 1.1 N/A N/A Details Liothyronine Thyroid hormone receptor alpha IC 50 (nM) 0.24 N/A N/A Details Liothyronine Thyroid hormone receptor beta IC 50 (nM) 0.26 N/A N/A Details