217302-87-9Relevant academic research and scientific papers
Synthesis and estrogen receptor binding affinities of novel pyrrolo[2,1,5-cd]indolizine derivatives
Jorgensen, Anker Steen,Jacobsen, Poul,Christiansen, Lise Brown,Bury, Paul S.,Kanstrup, Anders,Thorpe, Susan M.,Narum, Lars,Wassermann, Karsten
, p. 2383 - 2386 (2007/10/03)
A series of pyrrolo[2,1,5-cd]indolizine derivatives has been synthesized and evaluated as ligands for the estrogen receptor. Properly substituted mono- and di-hydroxy derivatives showed binding in the low nanomolar range in accordance with their structural resemblance to estrogen. (C) 2000 Elsevier Science Ltd.
Pyrrolo[2,1,5-cd]indolizine derivatives useful in the prevention or treatment of estrogen related diseases or syndromes
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, (2008/06/13)
The present invention relates to therapeutically active compounds of formula I a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in the prevention or treatment of estrogen related diseases or syndromes.
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
Jorgensen,Jacobsen,Christiansen,Bury,Kanstrup,Thorpe,Bain,Naerum,Wassermann
, p. 399 - 402 (2007/10/03)
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.
