✦ LIBER ✦

Conversion of the phytoestrogen coumestrol into a selective estrogen receptor modulator (SERM) by attachment of an amine-containing sidechain

✍ Scribed by Timothy A. Grese; Harlan W. Cole; David E. Magee; D. Lynn Phillips; Pam K. Shetler; Lorri L. Short; Andrews L. Glasebrook; Henry U. Bryant

Publisher: Elsevier Science
Year: 1996
Tongue: English
Weight: 222 KB
Volume: 6
Category: Article
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(96)00502-1

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✦ Synopsis

The naturally occurring estrogen mimetic coumestrol has been shown to stimulate proliferation of MCF-7 mammary tumor cells and to cause uterotrophic effects in ovariectomized (OVX) rats. Attachment of a basic amine-containing sidechain to C-6 of coumestrol converts this estrogen agonist into an antagonist in breast and uterine tissue, while maintaining its estrogen-like activity as a hypocholesterolemic agent.