Synthesis and estrogen receptor binding affinities of novel pyrrolo[2,1,5- cd]indolizine derivatives

Synthesis and estrogen receptor binding affinities of novel pyrrolo[2,1,5- cd]indolizine derivatives

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.

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2000-10, Vol.10 (20), p.2383-2386
Hauptverfasser: Jørgensen, Anker Steen, Jacobsen, Poul, Christiansen, Lise Brown, Bury, Paul S., Kanstrup, Anders, Thorpe, Susan M., Nærum, Lars, Wassermann, Karsten
Format: Artikel
Sprache:eng
Schlagworte:
Biological and medical sciences
Drug Design
Estradiol - metabolism
Hormones. Endocrine system
Humans
Indolizines - chemical synthesis
Indolizines - chemistry
Indolizines - pharmacokinetics
Kinetics
Medical sciences
Models, Molecular
Molecular Conformation
Molecular Structure
Pharmacology. Drug treatments
Pyrroles - chemical synthesis
Pyrroles - chemistry
Pyrroles - pharmacokinetics
Receptors, Estrogen - metabolism
Structure-Activity Relationship
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Zusammenfassung: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00474-1