Thyroid receptor ligands. Part 7: Indirect antagonists of the thyroid hormone receptor with improved affinity

Sammanfattning

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.

Nyckelord

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

Publicerad i

Bioorganic and Medicinal Chemistry Letters
2007, volym: 17, nummer: 7, sidor: 2018-2021
Utgivare: PERGAMON-ELSEVIER SCIENCE LTD

SLU författare

• Agback, Peter

  • Karo Bio AB

UKÄ forskningsämne

Organisk kemi

Publikationens identifierare

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

Permanent länk till denna sida (URI)

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