660409-78-9Relevant academic research and scientific papers
Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: Potent, TRβ subtype-selective thyromimetics
Dow, Robert L.,Schneider, Steven R.,Paight, Ernest S.,Hank, Richard F.,Chiang, Phoebe,Cornelius, Peter,Lee, Eunsun,Newsome, William P.,Swick, Andrew G.,Spitzer, Josephine,Hargrove, Diane M.,Patterson, Terrell A.,Pandit, Jayvardhan,Chrunyk, Boris A.,LeMotte, Peter K.,Danley, Dennis E.,Rosner, Michele H.,Ammirati, Mark J.,Simons, Samuel P.,Schulte, Gayle K.,Tate, Bonnie F.,DaSilva-Jardine, Paul
, p. 379 - 382 (2007/10/03)
In this communication, we wish to describe the discovery of a novel series of 6-azauracil-based thyromimetics that possess up to 100-fold selectivities for binding and functional activation of the β1-isoform of the thyroid receptor family. Structure-activity relationship studies on the 3,5- and 3′-positions provided compounds with enhanced TRβ affinity and selectivity. Key binding interactions between the 6-azauracil moiety and the receptor have been determined through of X-ray crystallographic analysis.
