Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4-alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor

Hedfors A, Appelqvist T, Carlsson B, Bladh LG, Litten C, Agback P, Grynfarb M, Koehler KF, Malm J

doi:10.1021/jm050004k

Research article2005Peer reviewed

Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4-alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor

Hedfors A, Appelqvist T, Carlsson B, Bladh LG, Litten C, Agback P, Grynfarb M, Koehler KF, Malm J

Abstract

Based on the recently described concept of "indirect antagonism" of nuclear receptors, a series of thyroid hormone receptor (TR) antagonists were prepared, in which the outer ring of a thyromimetic was replaced with alkyl chains of variable length and branch. The results of a binding assay for the human TR and reporter cell assay revealed, within this series, a positive correlation between increasing bulk of the alkyl group and affinity to TRs. Compared with already reported TR antagonists, their affinities are within the same range, thus potentially representing a useful approach to novel and high affinity TR-antagonists.

Published in

Journal of Medicinal Chemistry
2005, Volume: 48, number: 9, pages: 3114-3117
Publisher: AMER CHEMICAL SOC

UKÄ Subject classification

Organic Chemistry

Publication identifier

DOI: https://doi.org/10.1021/jm050004k

Permanent link to this page (URI)

https://res.slu.se/id/publ/83905