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

Johan Malm; Sandra Gordon; Peter Brandt; Bo Carlsson; Peter Agback; Anna Bäckbro Saeidi; Johnny Sandberg

doi:10.1016/j.bmcl.2007.01.009

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

Johan Malm
, Sandra Gordon
, Peter Brandt
, Bo Carlsson
, Peter Agback
, Anna Bäckbro Saeidi
, Johnny Sandberg

Publikation: Bidrag till tidskrift › Artikel i vetenskaplig tidskrift › Peer review

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.

Originalspråk	Engelska
Sidor (från-till)	2018-2021
Antal sidor	4
Tidskrift	Bioorganic and Medicinal Chemistry Letters
Volym	17
Nummer	7
DOI	https://doi.org/10.1016/j.bmcl.2007.01.009
Status	Publicerad - 2007
Externt publicerad	Ja

Nyckelord

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

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10.1016/j.bmcl.2007.01.009

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

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.",

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author = "Johan Malm and Sandra Gordon and Peter Brandt and Bo Carlsson and Peter Agback and \{B{\"a}ckbro Saeidi\}, Anna and Johnny Sandberg",

year = "2007",

doi = "10.1016/j.bmcl.2007.01.009",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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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.

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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

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DO - 10.1016/j.bmcl.2007.01.009

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JO - Bioorganic and Medicinal Chemistry Letters

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