Synthesis and evaluation of hexahydrochrysene and tetrahydrobenzofluorene ligands for the estrogen receptor.
To prepare novel estrogen receptor (ER) ligands, we have developed a facile approach to substituted hexahydrochrysene and tetrahydrobenzo[a]fluorene systems. Substituents, including basic side chains, were added to these systems, and their binding affinity to ERalpha and ERbeta, and in some cases their transcriptional activity were evaluated.
Tedesco
R
R
Department of Chemistry, University of Illinois, Urbana 61801, USA.
Youngman
M K
MK
Wilson
S R
SR
Katzenellenbogen
J A
JA
D002911:Chrysenes / Q000138:chemical synthesis* / Q000494:pharmacology; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D005449:Fluorenes / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D008024:Ligands; D008968:Molecular Conformation; D011083:Polycyclic Compounds / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology; D011485:Protein Binding; D011960:Receptors, Estrogen / Q000819:agonists / Q000037:antagonists & inhibitors / Q000187:drug effects* / Q000378:metabolism; D013329:Structure-Activity Relationship; D014158:Transcription, Genetic / Q000187:drug effects; D014407:Tumor Cells, Cultured / Q000187:drug effects
D002911:Chrysenes; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D005449:Fluorenes; D008024:Ligands; D011083:Polycyclic Compounds; D011960:Receptors, Estrogen; C444840:hexahydrochrysene; C444841:tetrahydrobenzofluorene