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Thyroid receptor ligands. Part 5: novel bicyclic agonist ligands selective for the thyroid hormone receptor beta.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 Mar 01; Vol. 16 (5), pp. 1240-4. Date of Electronic Publication: 2005 Dec 09. - Publication Year :
- 2006
-
Abstract
- Based on the examination of the crystal structure of rat TRbeta complexed with 3,5,3'-triiodo-l-thyronine (2) a novel TRbeta-selective indole derivative 6b was prepared and tested in vitro. This compound was found to be 14 times selective for TRbeta over TRalpha in binding and its beta-selectivity could be rationalized through the comparison of the X-ray crystallographic structures of 6b complexed with TRalpha and TRbeta.
- Subjects :
- Animals
Crystallography, X-Ray
Cyclization
Humans
Indoles metabolism
Inhibitory Concentration 50
Ligands
Molecular Structure
Rats
Substrate Specificity
Thyroid Hormone Receptors beta chemistry
Thyroxine chemical synthesis
Thyroxine chemistry
Indoles chemistry
Indoles pharmacology
Thyroid Hormone Receptors beta agonists
Thyroid Hormone Receptors beta metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 16
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 16338239
- Full Text :
- https://doi.org/10.1016/j.bmcl.2005.11.077