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Bioorg Med Chem Lett. 2004 May 17;14(10):2551-4.

Estrogen receptor ligands. Part 3: The SAR of dihydrobenzoxathiin SERMs.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. helen_chen@merck.com

Abstract

A series of 3-alkyl, 3-cycloalkyl, and 3-heteroaryl dihydrobenzoxathiin analogs 1 were prepared and evaluated for estrogen/anti-estrogen activity in both in vitro and in vivo models. In general, the compounds were found to exhibit a high degree of selectivity for ER alpha over ER beta, but were less potent than the original lead compound 1a in the inhibition of estradiol-driven uterine proliferation.

PMID:
15109649
DOI:
10.1016/j.bmcl.2004.02.084
[Indexed for MEDLINE]

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