Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity

被引：52

作者：

Chen, HY

Dykstra, KD

Birzin, ET

Frisch, K

Chan, W

Yang, YT

Mosley, RT

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 06期

关键词：

SERMs; flavanoids;

D O I：

10.1016/j.bmcl.2004.01.031

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A class of flavanoids exhibiting a high degree of selectivity for ERalpha over ERbeta has been discovered. The most active analogue 6 was found to be 66-fold ERalpha-selective and demonstrated uterine estradiol antagonism. (C) 2004 Elsevier Ltd. All rights reserved.

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收藏

页码：1417 / 1421

页数：5

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