Search | VHL Regional Portal

Synthesis and evaluation of hexahydrochrysene and tetrahydrobenzofluorene ligands for the estrogen receptor.

Tedesco, R; Youngman, M K; Wilson, S R; Katzenellenbogen, J A.

Bioorg Med Chem Lett ; 11(10): 1281-4, 2001 May 21.

Article in English | MEDLINE | ID: mdl-11392537

ABSTRACT

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.

Subject(s)

Chrysenes/chemical synthesis , Fluorenes/chemical synthesis , Receptors, Estrogen/drug effects , Chrysenes/pharmacology , Estrogen Receptor alpha , Estrogen Receptor beta , Fluorenes/pharmacology , Humans , Ligands , Molecular Conformation , Polycyclic Compounds/chemical synthesis , Polycyclic Compounds/metabolism , Polycyclic Compounds/pharmacology , Protein Binding , Receptors, Estrogen/agonists , Receptors, Estrogen/antagonists & inhibitors , Receptors, Estrogen/metabolism , Structure-Activity Relationship , Transcription, Genetic/drug effects , Tumor Cells, Cultured/drug effects

ABSTRACT

Subject(s)

SEND TO:

SELECTION OF CITATIONS

SEARCH DETAIL