The modulation of gene regulation by blocking the interaction between the thyroid receptor (TR) and obligate coregulators has been reported recently with the discovery of the lead compound 3-(dimethylamino)-1-(4-hexylphenyl) propan-1-one). Herein we report studies aimed at optimization of this initial hit to determine the basic parameters of the structure- activity relationships and clarify the mechanism of action. These studies provided new ...
