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

A S Jørgensen; P Jacobsen; L B Christiansen; P S Bury; A Kanstrup; S M Thorpe; L Naerum; K Wassermann

doi:10.1016/s0960-894x(00)00474-1

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

Bioorg Med Chem Lett. 2000 Oct 16;10(20):2383-6. doi: 10.1016/s0960-894x(00)00474-1.

Authors

A S Jørgensen¹, P Jacobsen, L B Christiansen, P S Bury, A Kanstrup, S M Thorpe, L Naerum, K Wassermann

Affiliation

¹ Health Care Discovery and Preclinical Development, Novo Nordisk A/S, Målov, Denmark. asj@novo.dk

PMID: 11055361
DOI: 10.1016/s0960-894x(00)00474-1

Abstract

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.

MeSH terms

Drug Design
Estradiol / metabolism
Humans
Indolizines / chemical synthesis*
Indolizines / chemistry
Indolizines / pharmacokinetics
Kinetics
Models, Molecular
Molecular Conformation
Molecular Structure
Pyrroles / chemical synthesis*
Pyrroles / chemistry
Pyrroles / pharmacokinetics
Receptors, Estrogen / metabolism*
Structure-Activity Relationship

Substances

Indolizines
Pyrroles
Receptors, Estrogen
Estradiol