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Synthesis and biological evaluation of stilbene-based pure estrogen antagonists

Walter, Georg ; Liebl, Renate ; Angerer, Erwin von



Abstract

Replacement of one of the ethyl substituents in diethylstilbestrol by side chains with functional groups converted this potent estrogen into pure antiestrogens with the potential for the treatment of breast cancer. These agents completely suppressed estrogen receptor-mediated gene activation and inhibited the growth of estrogen-sensitive MCF-7 breast cancer cells in submicromolar concentrations. ...

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