Exploration of the bicyclo[3.3.1]nonane system as a template for the development of new ligands for the estrogen receptor.
Three novel structural motifs based on a bicyclo [3.3.1]nonane template were examined as new ligands for estrogen receptor (ER). Type III compounds emerged as the most promising leads for developing high-affinity ER ligands, but they showed little selectivity for either ER subtype. Type II compounds, on the other hand, despite their lower affinity, exhibited significant ERbeta binding selectivity.
Muthyala
Rajeev S
RS
Department of Chemistry, University of Illinois, 600 S Mathews Avenue, Urbana, IL 61801, USA.
Carlson
Kathryn E
KE
Katzenellenbogen
John A
JA
D000473:Alkanes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D001643:Bridged Bicyclo Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001952:Bridged-Ring Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D003506:Cyclofenil / Q000378:metabolism; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D005260:Female; D007202:Indicators and Reagents; D007700:Kinetics; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D011869:Radioligand Assay; D011960:Receptors, Estrogen / Q000187:drug effects / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
D000473:Alkanes; D001643:Bridged Bicyclo Compounds; D001952:Bridged-Ring Compounds; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D007202:Indicators and Reagents; D008024:Ligands; D011960:Receptors, Estrogen; C458301:bicyclo(3.3.1)nonane; D003506:Cyclofenil; C017573:nonane