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Bioorg Med Chem Lett. 2005 Feb 1;15(3):715-8.

Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans.

Author information

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

Abstract

The ring oxygen and sulfur analogs of lasofoxifene, 1a and 1b, were synthesized in an attempt to impart ERalpha selectivity, as found in the closely related dihydrobenzoxathiin compound I, recently discovered in these laboratories. The resulting isochroman and isothiochroman compounds were found to exhibit equipotent binding affinities to the ER isoforms and were less active in the inhibition of estradiol-triggered uterine growth when compared to I and lasofoxifene.

PMID:
15664843
DOI:
10.1016/j.bmcl.2004.11.018
[Indexed for MEDLINE]

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