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

Authors
Jorgensen, AS Jacobsen, P Christiansen, LB Bury, PS Kanstrup, A Thorpe, SM Bain, S Naerum, L Wassermann, K
Citation
As. Jorgensen et al., 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, BIOORG MED, 10(4), 2000, pp. 399-402
Citations number
20
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
4
Year of publication
2000
Pages
399 - 402
Database
ISI
SICI code
0960-894X(20000221)10:4<399:SAPOAN>2.0.ZU;2-V
Abstract
1-Ethyl-2-(4-hydroxyphenyl)pyrrolo[2,1,5-cd]indolizine (NNC 45-0095) is a n ovel compound which represents the parent pharmacophore structure of a seri es of pyrrolo[2,1,5-cd]indolizine derivatives with mixed estrogen agonist/a ntagonist 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 o variectomized mouse model for post-menopausal osteoporosis. (C) 2000 Elsevi er Science Ltd. All rights reserved.