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 ERα and ERβ, and in some cases their transcriptional activity were evaluated.