Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives

被引：13

作者：

Miller, CP

Jirkovsky, I

Tran, BD

Harris, HA

Moran, RA

Komm, BS

机构：

[1] Wyeth Ayerst Res, Womens Hlth Res Inst, Radnor, PA 19087 USA

[2] Wyeth Ayerst Res & Dev, Pearl River, NY 10965 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(99)00648-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A diastereomerically pure series of 7 alpha-thioestratrienes was prepared and evaluated for its affinity for both the human estrogen receptor alpha and the more recently discovered estrogen receptor beta. The functional estrogenic activities of the compounds were measured in a MCF-7 ERE-tk-luciferase assay. The activities and selectivities of the compounds were sensitive to the nature of the thioether side chain. (C) 2000 Elsevier Science Ltd. All rights reserved.

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页码：147 / 151

页数：5

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