CONVERSION OF THE PHYTOESTROGEN COUMESTROL INTO A SELECTIVE ESTROGEN-RECEPTOR MODULATOR (SERM) BY ATTACHMENT OF AN AMINE-CONTAINING SIDE-CHAIN

Authors
GRESE TA COLE HW MAGEE DE PHILLIPS DL SHETLER PK SHORT LL GLASEBROOK AL BRYANT HU
Citation
Ta. Grese et al., CONVERSION OF THE PHYTOESTROGEN COUMESTROL INTO A SELECTIVE ESTROGEN-RECEPTOR MODULATOR (SERM) BY ATTACHMENT OF AN AMINE-CONTAINING SIDE-CHAIN, Bioorganic & medicinal chemistry letters, 6(22), 1996, pp. 2683-2686
Citations number
23
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
22
Year of publication
1996
Pages
2683 - 2686
Database
ISI
SICI code
0960-894X(1996)6:22<2683:COTPCI>2.0.ZU;2-T
Abstract
The naturally occurring estrogen mimetic coumestrol has been shown to stimulate proliferation of MCF-7 mammary tumor cells and to cause uter otrophic effects in ovariectomized (OVX) rats. Attachment of a basic a mine-containing sidechain to C-6 of coumestrol converts this estrogen agonist into an antagonist in breast and uterine tissue, while maintai ning its estrogen-like activity as a hypocholesterolemic agent. Copyri ght (C) 1996 Elsevier Science Ltd