雌激素受体配体。第3部分：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 3: The SAR of dihydrobenzoxathiin SERMs.
作者信息
Chen Helen Y, Kim Seongkon, Wu Jane Y, Birzin Elizabeth T, Chan Wanda, Yang Yi Tien, 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, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2004 May 17;14(10):2551-4. doi: 10.1016/j.bmcl.2004.02.084.
A series of 3-alkyl, 3-cycloalkyl, and 3-heteroaryl dihydrobenzoxathiin analogs 1 were prepared and evaluated for estrogen/anti-estrogen activity in both in vitro and in vivo models. In general, the compounds were found to exhibit a high degree of selectivity for ER alpha over ER beta, but were less potent than the original lead compound 1a in the inhibition of estradiol-driven uterine proliferation.
制备了一系列3-烷基、3-环烷基和3-杂芳基二氢苯并噻吩类似物1，并在体外和体内模型中评估其雌激素/抗雌激素活性。总体而言，发现这些化合物对雌激素受体α（ERα）的选择性高于雌激素受体β（ERβ），但在抑制雌二醇驱动的子宫增殖方面比原始先导化合物1a的效力更低。
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