Furans with basic side chains: synthesis and biological evaluation of a novel series of antagonists with selectivity for the estrogen receptor alpha.
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.
Mortensen
D S
DS
Department of Chemistry, University of Illinois, Urbana, 61801, USA.
Rodriguez
A L
AL
Sun
J
J
Katzenellenbogen
B S
BS
Katzenellenbogen
J A
JA
D002478:Cells, Cultured; D018360:Crystallography, X-Ray; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D020847:Estrogen Receptor Modulators / Q000737:chemistry* / Q000494:pharmacology*; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D005260:Female; D005663:Furans / Q000737:chemistry; D006801:Humans; D015394:Molecular Structure; D011960:Receptors, Estrogen / Q000037:antagonists & inhibitors* / Q000187:drug effects; D013329:Structure-Activity Relationship
D020847:Estrogen Receptor Modulators; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D005663:Furans; D011960:Receptors, Estrogen