Document Report Card

ID: ALA1143623

Journal: J Med Chem

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

Authors: 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.

CiteXplore: 15857115

DOI: 10.1021/jm050004k