Structure-property and structure-activity relationships of bisphenol derivatives as estrogen receptor modulators

抄録

Bisphenols show endocrine-disrupting activity by modulating nuclear receptors such as estrogen receptors (ERs) and estrogenrelated receptors, and are long-term environmental pollutants. In this study, we investigated the physicochemical properties and activities towards ERα and ERβ of bisphenol derivatives with diverse linking structures. The potency and mode of activity towards ERs, i.e., agonistic or antagonistic, was found to depend strongly on the linking structure between the two phenolic groups. The obtained structure-property and structure-activity relationships should be helpful both in understanding the effects of environmental pollution by endocrine-disrupting chemicals and in developing ER-targeting drug candidates, such as anticancer drugs.