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Bioorg Med Chem Lett. 2004 Jul 16;14(14):3753-5.

Estrogen receptor ligands. Part 6: Synthesis and binding affinity of dihydrobenzodithiins.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, 800B-107, Rahway, NJ 07065, USA. qiang_tan@merck.com

Abstract

Dihydrobenzodithiin compounds (1-6) were prepared to explore the expansion of the dihydrobenzoxathiin lead compounds I-III as SERAMs (Selective Estrogen Receptor Alpha Modulators). The dihydrobenzodithiin compounds generally maintained a high degree of selectivity for ERalpha over ERbeta, however, they lacked the in vivo antagonism/agonism activity exhibited by the lead class in an immature rat uterine growth model.

PMID:
15203156
DOI:
10.1016/j.bmcl.2004.04.101
[Indexed for MEDLINE]

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