Document Report Card

Basic Information

ID: ALA1138993

Journal: Bioorg Med Chem Lett

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

Authors: Garcia Collazo AM, Koehler KF, Garg N, Färnegårdh M, Husman B, Ye L, Ljunggren J, Mellström K, Sandberg J, Grynfarb M, Ahola H, Malm J.

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.

CiteXplore: 16338239

DOI: 10.1016/j.bmcl.2005.11.077