TY - JOUR
T1 - Thyroid receptor ligands. Part 7: Indirect antagonists of the thyroid hormone receptor with improved affinity
AU - Malm, Johan
AU - Gordon, Sandra
AU - Brandt, Peter
AU - Carlsson, Bo
AU - Agback, Peter
AU - Bäckbro Saeidi, Anna
AU - Sandberg, Johnny
PY - 2007
Y1 - 2007
N2 - 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.
AB - 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.
KW - thyroid hormone receptor
KW - thyroid hormone antagonist
KW - indirect antagonism
KW - benzyloxyphenyl derivatives
KW - thyroid hormone agonist
KW - thyrotoxicosis
KW - hyperthyroidism
KW - thyroid hormone receptor
KW - thyroid hormone antagonist
KW - indirect antagonism
KW - benzyloxyphenyl derivatives
KW - thyroid hormone agonist
KW - thyrotoxicosis
KW - hyperthyroidism
UR - https://res.slu.se/id/publ/83872
U2 - 10.1016/j.bmcl.2007.01.009
DO - 10.1016/j.bmcl.2007.01.009
M3 - Journal article
C2 - 17254783
SN - 0960-894X
VL - 17
SP - 2018
EP - 2021
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 7
ER -