新型、选择性非甾体糖皮质激素受体拮抗剂的合成与生物学评价
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
作者信息
Akritopoulou-Zanze Irini, Patel Jyoti R, Hartandi Kresna, Brenneman Jehrod, Winn Martin, Pratt John K, Grynfarb Marlene, Goos-Nisson Annika, Von Geldern Thomas W, Kym Philip R
机构信息
Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60044, USA.
出版信息
Bioorg Med Chem Lett. 2004 May 3;14(9):2079-82. doi: 10.1016/j.bmcl.2004.02.048.
PMID:15080982
Abstract
We report the discovery of a novel class of glucocorticoid receptor (GR) antagonists based on the chromene molecular scaffold. The compounds exhibit good functional potency and an improved receptor selectivity profile for GR over other steroid receptors when compared to the classical steroidal GR-antagonist, RU-486.
摘要
我们报告了基于色烯分子支架发现的一类新型糖皮质激素受体（GR）拮抗剂。与经典甾体GR拮抗剂RU-486相比，这些化合物表现出良好的功能效力，并且对GR的受体选择性优于其他甾体受体。
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