Abstract

Based on the concept of 'indirect antagonism' of nuclear receptors, a series of thyroid hormone receptor (TR) antagonists were prepared with improved affinity compared with what was previously described. The results of a binding assay for the human TR and reporter cell assay revealed, within this series, that an m-bromobenzoyl substituent (11f) was optimal in terms of affinity and antagonist activity. Compared with already reported TR antagonists, their affinities are within the same range, thus potentially representing useful approach to novel and high-affinity TR-antagonists. (c) 2007 Elsevier Ltd. All rights reserved.

Keywords

thyroid hormone receptor; thyroid hormone antagonist; indirect antagonism; benzyloxyphenyl derivatives; thyroid hormone agonist; thyrotoxicosis; hyperthyroidism

Published in

Bioorganic and Medicinal Chemistry Letters
2007, Volume: 17, number: 7, pages: 2018-2021
Publisher: PERGAMON-ELSEVIER SCIENCE LTD

UKÄ Subject classification

Organic Chemistry


Publication identifier

DOI: https://doi.org/10.1016/j.bmcl.2007.01.009

Permanent link to this page (URI)

https://res.slu.se/id/publ/83872