Synthesis and pharmacology of a novel pyrrolo[2,1,5-cd] indolizine (NNC 45-0095), a high affinity non-steroidal agonist for the estrogen receptor

被引：46
作者：
Jorgensen, AS
Jacobsen, P
Christiansen, LB
Bury, PS
Kanstrup, A
Thorpe, SM
Bain, S
Nærum, L
Wassermann, K
机构：
[1] Novo Nordisk AS, Hlth Care Discovery & Preclin Dev, DK-2760 Malov, Denmark
[2] SkeleTech Inc, Seattle, WA USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 04期
关键词：
D O I：
10.1016/S0960-894X(00)00015-9
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
1-Ethyl-2-(4-hydroxyphenyl)pyrrolo[2,1,5-cd]indolizine (NNC 45-0095) is a novel compound which represents the parent pharmacophore structure of a series of pyrrolo[2,1,5-cd]indolizine derivatives with mixed estrogen agonist/antagonist properties. NNC 45-0095 binds with high affinity to the estrogen receptor (IC50 = 9.5 nM) and exhibits full protection of bone loss in the ovariectomized mouse model for post-menopausal osteoporosis. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：399 / 402
页数：4
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