|
[摘要]:Highly TR beta selective thyromimetics have several potential therapeutic applications. Based on the novel indane derivative KTA-439 with high receptor (TR beta) and organ (liver) selectivity, a series of thyroid hormone analogues were prepared, in which the isopropyl at the 3'-position was replaced with alkyl and aralkyl moieties of variable lengths and branches. Binding assays for these human TRs and reporter cell assays showed that 2-arylethyl derivatives had higher TR beta selectivity than KTA-439. KTA-574, a representative 2-arylethyl derivative, had TR beta specificity in a binding assay and exhibited full agonism in a reporter cell assay. (C) 2012 Elsevier Ltd. All rights reserved. |
|