Furans with basic side chains: synthesis and biological evaluation of a novel series of antagonists with selectivity for the estrogen receptor alpha

D S Mortensen; A L Rodriguez; J Sun; B S Katzenellenbogen; J A Katzenellenbogen

doi:10.1016/s0960-894x(01)00488-7

Furans with basic side chains: synthesis and biological evaluation of a novel series of antagonists with selectivity for the estrogen receptor alpha

Bioorg Med Chem Lett. 2001 Sep 17;11(18):2521-4. doi: 10.1016/s0960-894x(01)00488-7.

Authors

D S Mortensen¹, A L Rodriguez, J Sun, B S Katzenellenbogen, J A Katzenellenbogen

Affiliation

¹ Department of Chemistry, University of Illinois, Urbana, 61801, USA.

PMID: 11549460
DOI: 10.1016/s0960-894x(01)00488-7

Abstract

3-alkyl-2,4,5-triarylfurans with basic side-chain substituents were prepared as ligands for the estrogen receptor. Those analogues having the basic side chain on the C(4) phenol were high-affinity, ERalpha-selective antagonists.

Publication types

Comparative Study
Evaluation Study
Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, Non-P.H.S.
Research Support, U.S. Gov't, P.H.S.

MeSH terms

Cells, Cultured
Crystallography, X-Ray
Dose-Response Relationship, Drug
Drug Design
Drug Evaluation, Preclinical
Estrogen Receptor Modulators / chemistry*
Estrogen Receptor Modulators / pharmacology*
Estrogen Receptor alpha
Estrogen Receptor beta
Female
Furans / chemistry
Humans
Molecular Structure
Receptors, Estrogen / antagonists & inhibitors*
Receptors, Estrogen / drug effects
Structure-Activity Relationship

Substances

Estrogen Receptor Modulators
Estrogen Receptor alpha
Estrogen Receptor beta
Furans
Receptors, Estrogen