We present and examine the efficacy of a novel benzoxepin-based scaffold for modulation of the human estrogen receptor. Receptor tolerance of this new molecular scaffold is examined through presentation of experimentally determined antiproliferative effects on human MCF-7 breast tumor cells and measured binding affinities. The effect of functional group substitution on the benzoxepin scaffold is explored through a brief computational structure - activity relationship investigation with molecular simulation.
Lloyd, D.G., Hughes, R.B., Zisterer, D.M., Williams, D.C., Fattorusso, C., Catalanotti, B., et al. (2004). Benzoxepin-derived estrogen receptor modulators: a novel molecular scaffold for the estrogen receptor. JOURNAL OF MEDICINAL CHEMISTRY, 47(23), 5612-5615 [10.1021/jm0495834].
Benzoxepin-derived estrogen receptor modulators: a novel molecular scaffold for the estrogen receptor
CAMPIANI G.;
2004-01-01
Abstract
We present and examine the efficacy of a novel benzoxepin-based scaffold for modulation of the human estrogen receptor. Receptor tolerance of this new molecular scaffold is examined through presentation of experimentally determined antiproliferative effects on human MCF-7 breast tumor cells and measured binding affinities. The effect of functional group substitution on the benzoxepin scaffold is explored through a brief computational structure - activity relationship investigation with molecular simulation.File | Dimensione | Formato | |
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https://hdl.handle.net/11365/8179
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