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.
MeSH terms
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Animals
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Aziridines / chemical synthesis*
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Aziridines / pharmacology
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Breast Neoplasms / pathology
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Chemical Phenomena
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Chemistry
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Female
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Fluorescent Dyes / chemical synthesis*
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Fluorescent Dyes / pharmacology
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Humans
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Indoles / chemical synthesis*
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Indoles / pharmacology
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Mice
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Receptors, Estrogen / drug effects*
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Tumor Cells, Cultured / drug effects
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Tumor Cells, Cultured / pathology
Substances
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Aziridines
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Fluorescent Dyes
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Indoles
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Receptors, Estrogen
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1-(6-aziridinylhexyl)-2-(4-hydroxyphenyl)indol-5-ol