雌激素受体配体。第4部分：顺式二氢苯并噻吩类选择性雌激素受体调节剂的构效关系
Estrogen receptor ligands. Part 4: The SAR of the syn-dihydrobenzoxathiin SERAMs.
作者信息
Kim Seongkon, Wu Jane, Chen Helen Y, Birzin Elizabeth T, Chan Wanda, Yang Yi Tien, Colwell Lawrence, Li Susan, Dahllund Johanna, DiNinno Frank, Rohrer Susan P, Schaeffer James M, Hammond Milton L
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, 800B-109, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2004 Jun 7;14(11):2741-5. doi: 10.1016/j.bmcl.2004.03.074.
A series of estrogen receptor ligands based on a dihydrobenzoxathiin scaffold is described and evaluated for estrogen/anti-estrogen activity in both in vitro and in vivo models. The most active analogue, 22, was found to be 40-fold ERalpha selective in a competitive binding assay, and 22 demonstrated very potent in vivo antagonism of estradiol driven proliferation in an immature rat uterine weight gain assay.
描述并评估了一系列基于二氢苯并噻吩支架的雌激素受体配体在体外和体内模型中的雌激素/抗雌激素活性。在竞争性结合试验中，活性最高的类似物22对雌激素受体α具有40倍的选择性，并且在未成熟大鼠子宫增重试验中，22对雌二醇驱动的增殖表现出非常强的体内拮抗作用。
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