Thyroid receptor ligands. Part 5: novel bicyclic agonist ligands selective for the thyroid hormone receptor beta.

Autor: Garcia Collazo AM; Karo Bio AB, Novum, Huddinge SE-141 57, Sweden., Koehler KF, Garg N, Färnegårdh M, Husman B, Ye L, Ljunggren J, Mellström K, Sandberg J, Grynfarb M, Ahola H, Malm J
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 Mar 01; Vol. 16 (5), pp. 1240-4. Date of Electronic Publication: 2005 Dec 09.
DOI: 10.1016/j.bmcl.2005.11.077
Abstrakt: 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.
Databáze: MEDLINE