Pyrazolo[1,5-a]pyrimidines as estrogen receptor ligands:: defining the orientation of a novel heterocyclic core

被引：28

作者：

Compton, DR ^{[1
]}

Carlson, KE ^{[1
]}

Katzenellenbogen, JA ^{[1
]}

机构：

[1] Univ Illinois, Dept Chem, Urbana, IL 61801 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 22期

关键词：

D O I：

10.1016/j.bmcl.2004.08.046

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have examined the pyrazolo[1,5-a]pyrimidine scaffold as a novel core structure for estrogen receptor ligands. Attachment of various substituents has helped to define the orientation of this heterocycle in the ligand-binding pocket as one in which a pendant phenol rather than the hydroxylpyrimidine serves as a mimic of the A-ring of estradiol. (C) 2004 Elsevier Ltd. All rights reserved.

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页码：5681 / 5684

页数：4

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