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Bioorg Med Chem Lett. 2004 Jun 7;14(11):2741-5.

Estrogen receptor ligands. Part 4: The SAR of the syn-dihydrobenzoxathiin SERAMs.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, 800B-109, Rahway, NJ 07065, USA. seongkon_kim@merck.com

Abstract

A series of estrogen receptor ligands based on a dihydrobenzoxathiin scaffold is described and evaluated for estrogen/anti-estrogen activity in both in vitro and in vivo models. The most active analogue, 22, was found to be 40-fold ERalpha selective in a competitive binding assay, and 22 demonstrated very potent in vivo antagonism of estradiol driven proliferation in an immature rat uterine weight gain assay.

PMID:
15125925
DOI:
10.1016/j.bmcl.2004.03.074
[Indexed for MEDLINE]

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