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Synthesis and Structure–Activity Relationships of a Class of Sodium Iodide Symporter Function Inhibitors
Author(s) -
Waltz Fanny,
Pillette Lucie,
Verhaeghe Elodie,
Ambroise Yves
Publication year - 2011
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201100258
Subject(s) - sodium iodide symporter , iodide , symporter , chemistry , thyroid , small molecule , thyroid function , computational biology , pharmacology , combinatorial chemistry , medicine , biochemistry , biology , organic chemistry , transporter , gene
Blocking iodide: Iodide capture plays a central role in many thyroid pathophysiological conditions. Here, we report the synthesis and biological evaluation of 184 N ‐benzylanilines as iodide transport inhibitors in thyroid‐derived cells. Important structure–activity relationships were elucidated, and two compounds with enhanced potency were identified. These new bioactive molecules are valuable pharmacological tools to further understand how iodide is captured in the thyroid, and the SAR data may prove useful for the development of novel antithyroid agents.