575504-18-6Relevant academic research and scientific papers
Design, synthesis, and structure-activity relationship (SAR) of N-[7-(4-hydroxyphenoxy)-6-methylindan-4-yl]malonamic acids as thyroid hormone receptor β (TRβ) selective agonists
Shiohara, Hiroaki,Nakamura, Tetsuya,Kikuchi, Norihiko,Ozawa, Tomonaga,Matsuzawa, Akane,Nagano, Ryuichi,Ohnota, Hideki,Miyamoto, Takahide,Ichikawa, Kazuo,Hashizume, Kiyoshi
, p. 592 - 607 (2013/02/25)
Highly TRβ selective thyromimetics have several potential therapeutic applications. Based on the novel indane derivative KTA-439 with high receptor (TRβ) 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 TRβ selectivity than KTA-439. KTA-574, a representative 2-arylethyl derivative, had TRβ specificity in a binding assay and exhibited full agonism in a reporter cell assay.
