| Literature DB >> 12565933 |
Robert L Dow1, Steven R Schneider, Ernest S Paight, Richard F Hank, Phoebe Chiang, Peter Cornelius, Eunsun Lee, William P Newsome, Andrew G Swick, Josephine Spitzer, Diane M Hargrove, Terrell A Patterson, Jayvardhan Pandit, Boris A Chrunyk, Peter K LeMotte, Dennis E Danley, Michele H Rosner, Mark J Ammirati, Samuel P Simons, Gayle K Schulte, Bonnie F Tate, Paul DaSilva-Jardine.
Abstract
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 beta(1)-isoform of the thyroid receptor family. Structure-activity relationship studies on the 3,5- and 3'-positions provided compounds with enhanced TR beta affinity and selectivity. Key binding interactions between the 6-azauracil moiety and the receptor have been determined through of X-ray crystallographic analysis.Entities:
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Year: 2003 PMID： 12565933 DOI： 10.1016/s0960-894x(02)00947-2
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823