Estrogen receptor ligands.: Part 4:: The SAR of the syn-dihydrobenzoxathiin SERAMs

被引：34

作者：

Kim, S

Wu, J

Chen, HY

Birzin, ET

Chan, WD

Yang, YT

Colwell, L

Li, S

Dahllund, J

DiNinno, F

Rohrer, SP

Schaeffer, JM

Hammond, ML

机构：

[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck Res Labs, Dept Atherosclerosis & Endocrinol, Rahway, NJ 07065 USA

[3] Kar Biol AB, Novum, S-14157 Huddinge, Sweden

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 11期

关键词：

SERM; benzoxathiin; estrogen;

D O I：

10.1016/j.bmcl.2004.03.074

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2004 Elsevier Ltd. All rights reserved.

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页码：2741 / 2745

页数：5

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