Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor β (TR-β) selective ligands
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- 作者：Saurin Raval ; Preeti Raval ; Debdutta B ; yopadhyay ; Krunal Soni ; Digambar Yevale ; Digvijay Jogiya ; Honey Modi ; Amit Joharapurkar ; Neha G ; hi ; Mukul R. Jain ; Pankaj R. Patel
- 关键词：3-Hydroxy-cyclobut-3-ene-1 ; 2-dione ; Thyroid hormone receptor ; TR-β ; Selective ; Squaric acid ; Thyroid receptor assay
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2008
- 出版时间：15 July 2008
- 年：2008
- 卷：18
- 期：14
- 页码：3919-3924
- 全文大小：313 K
文摘
Design and synthesis of a novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives are reported and their in vitro thyroid hormone receptor selectivity has been evaluated in the thyroid luciferase receptor assay. The 3-[3,5-dichloro-4-(4-hydroxy-3-isopropylphenoxy)-phenylamino]-4-hydroxy-cyclobut-3-ene-1,2-dione 21 has shown selectivity towards thyroid hormone receptor β.