Raval Saurin, Raval Preeti, Bandyopadhyay Debdutta, Soni Krunal, Yevale Digambar, Jogiya Digvijay, Modi Honey, Joharapurkar Amit, Gandhi Neha, Jain Mukul R, Patel Pankaj R
Zydus Research Centre, Medicinal Chemistry, Sarkhej-Bavla N. H.8A, Moraiya, Ahmedabad, Gujarat 382210, India.
Bioorg Med Chem Lett. 2008 Jul 15;18(14):3919-24. doi: 10.1016/j.bmcl.2008.06.038. Epub 2008 Jun 14.
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 beta.
报道了一种新型3-羟基-环丁-3-烯-1,2-二酮衍生物的设计与合成,并通过甲状腺荧光素酶受体测定法评估了它们的体外甲状腺激素受体选择性。3-[3,5-二氯-4-(4-羟基-3-异丙基苯氧基)-苯基氨基]-4-羟基-环丁-3-烯-1,2-二酮21已显示出对甲状腺激素受体β的选择性。