New clicked full agonists of the estrogen receptor β?
RSC Advances Pub Date: 2013-01-11 DOI: 10.1039/C3RA00122A
Abstract
A click chemistry approach was used to synthesize a series of 1,4-diaryl-substituted 1,2,3-triazoles designed to behave as estrogen receptor (ER) ligands. We studied their affinities for both receptors α and β, their agonist activities in a cell-based luciferase reporter assay and their effect on the proliferation of the hormone-dependent MCF-7 cell line. We found two compounds (3a and 3c) that behave as selective full agonists for ERβ at a 20 μM concentration, and one of them (3c) showed no proliferative effect on MCF-7 cells.
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Journal Name:RSC Advances
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CAS no.: 89640-58-4