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ID: ALA1136115
Journal: Bioorg Med Chem Lett
Title: Constrained phytoestrogens and analogues as ERbeta selective ligands.
Authors: Miller CP, Collini MD, Harris HA.
Abstract: A new series of ERbeta (ERbeta) selective ligands has been prepared. One of the compounds 6, structurally related to the phytoestrogen apigenin 4, displays a binding preference for ERbeta over ERalpha of over 40-fold. In addition to its binding selectivity, 6 was able to potently induce metallothionein (an ERbeta specific response in human SAOS-2 cells) while demonstrating low potency in an ERalpha dependant ERE-tk luciferase assay in MCF-7 cells. Such receptor and cell selectivity could make 6 a useful molecular probe for better understanding the role of ERbeta in mammalian physiology.
CiteXplore: 12824043