Bioorganic & medicinal chemistry letters

Constrained phytoestrogens and analogues as ERβ selective ligands

CP Miller, MD Collini, HA Harris

文献索引：Miller, Chris P.; Collini, Michael D.; Harris, Heather A. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 14 p. 2399 - 2403

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被引用次数: 45

摘要

A new series of ERbeta (ERβ) selective ligands has been prepared. One of the compounds 6, structurally related to the phytoestrogen apigenin 4, displays a binding preference for ERβ over ERα of over 40-fold. In addition to its binding selectivity, 6 was able to potently induce metallothionein (an ERβ specific response in human SAOS-2 cells) while demonstrating low potency in an ERα dependant ERE-tk luciferase assay in MCF-7 cells. Such receptor and ...