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2004
Polyphenylalkene derivatives
Q 0740
Synthesis and Biological Evaluation of Stilbene-Based Pure Estrogen Antagonists.
The potent estrogen diethylstilbestrol is converted into pure antiestrogens by replac50- 059 —
ing one of its ethyl groups with long alkyl chains bearing functional groups. The most
favorable substitution for achieving antagonism include the introduction of a tertiary
amino group in the side chain, separated by a hexamethylene spacer from the stilbene
core, an additional thio ether function, and a fluorinated terminal alkyl group as exemplified with (VIII). The antiestrogens completely suppress estrogen receptor mediated
gene activation and inhibit the growth of estrogen-sensitive MCF-7 breast cancer cells
in submicromolar concentrations. Agent (VIII) and the steroidal reference drug fulvestrant display similar activity both in vitro and in vivo. — (WALTER, G.; LIEBL, R.;
VON ANGERER*, E.; Bioorg. Med. Chem. Lett. 14 (2004) 18, 4659-4663;
Lehrstuhl Pharm. Chem. II, Inst. Pharm., Univ. Regensburg, D-93040 Regensburg,
Germany; Eng.) — H. Hoennerscheid
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