雌激素受体配体。第6部分：二氢苯并二硫醚的合成与结合亲和力。
Estrogen receptor ligands. Part 6: Synthesis and binding affinity of dihydrobenzodithiins.
作者信息
Tan Qiang, Birzin Elizabeth T, Chan Wanda, Yang Yi Tien, Pai Lee-Yuh, Hayes Edward C, DaSilva Carolyn A, 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-107, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2004 Jul 16;14(14):3753-5. doi: 10.1016/j.bmcl.2004.04.101.
Dihydrobenzodithiin compounds (1-6) were prepared to explore the expansion of the dihydrobenzoxathiin lead compounds I-III as SERAMs (Selective Estrogen Receptor Alpha Modulators). The dihydrobenzodithiin compounds generally maintained a high degree of selectivity for ERalpha over ERbeta, however, they lacked the in vivo antagonism/agonism activity exhibited by the lead class in an immature rat uterine growth model.
制备二氢苯并二硫醚化合物（1 - 6）以探索作为选择性雌激素受体α调节剂（SERAMs）的二氢苯并氧硫杂环化合物I - III的扩展。二氢苯并二硫醚化合物通常对雌激素受体α（ERα）比对雌激素受体β（ERβ）保持高度选择性，然而，它们在未成熟大鼠子宫生长模型中缺乏先导化合物类所表现出的体内拮抗/激动活性。
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