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2005
Benzofuran derivatives
R 0070
7-Substituted 2-Phenyl-benzofurans as ERβ Selective Ligands. — To increase the
of a benzofuranol derivative with potent binding affinity for ERβ, but which
01- 095 selectivity
lacks any group that could mimic the 5-OH group of genistein, analogues of this compound are synthesized containing relatively lipophilic groups at the benzofuran 7-position. Furthermore, several compounds with a fluoro group at the 2-phenyl group are
prepared. Incorporating additional groups at the 4-position of the benzofuran moiety
further increases selectivity for ERβ over ERα. Compounds (VIb) and (VII) are the
most selective ones of the series, with more than 100-fold selectivity for ERβ. Crystallography and molecular-modeling studies demonstrate that the benzofuran 7-position
plays a key role in the enhancement of ERβ selectivity (no yields given). —
(COLLINI*, M. D.; KAUFMAN, D. H.; MANAS, E. S.; HARRIS, H. A.;
HENDERSON, R. A.; XU, Z. B.; UNWALLA, R. J.; MILLER, C. P.; Bioorg. Med.
Chem. Lett. 14 (2004) 19, 4925-4929; Chem. Screening Sci., Wyeth Res. Ltd., Collegeville, PA 19426, USA; Eng.) — H. Hoennerscheid
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