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Synthesis and biological properties of a 1-(6-aziridinylhexyl)-2-phenylindole, a potential fluorescence label for estrogen receptors

Erber, S. ; Birnböck, H. ; Angerer, E. von



Abstract

2-Phenylindole derivative 8, linked to aziridine by a hexamethylene spacer group, was synthesized and tested. It binds to the estrogen receptor with an RBA-value of 4.0 (estradiol = 100). In vitro, it shows a selective cytostatic activity in hormone-dependent MCF-7 breast cancer cells (41% T/C at 10(-6) M). In vivo, it exerts a strong estrogenic effect. The binding to the estrogen receptor is largely reversible.


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