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Bioorg Med Chem Lett. 2002 Oct 21;12(20):2875-8.

Solid-phase synthesis and investigation of benzofurans as selective estrogen receptor modulators.

Author information

1
Department of Chemistry Research, Bayer Research Center, 400Morgan Lane, West Haven, CT 06516, USA.

Abstract

A library of benzofurans was prepared by solid-phase synthesis methods, and several analogues were identified as potent ligands for the estrogen receptors ER-alpha and ER-beta, with some compounds having selectivity for ER-alpha. Analogues designed to more closely mimic Raloxifene were less effective. Certain benzofurans were effective in a bone pit assay, but were characterized as agonists in a MCF-7 breast tumor cell proliferation assay.

PMID:
12270167
DOI:
10.1016/s0960-894x(02)00613-3
[Indexed for MEDLINE]

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