185254-74-4Relevant academic research and scientific papers
Synthesis and pharmacology of conformationally restricted raloxifene analogues: Highly potent selective estrogen receptor modulators
Grese, Timothy A.,Pennington, Lewis D.,Sluka, James P.,Dee Adrian,Cole, Harlan W.,Fuson, Tina R.,Magee, David E.,Lynn Phillips,Rowley, Ellen R.,Shetler, Pamela K.,Short, Lorri L.,Venugopalan, Murali,Yang, Na N.,Sato, Masahiko,Glasebrook, Andrew L.,Bryant, Henry U.
, p. 1272 - 1283 (2007/10/03)
The 2-arylbenzothiophene raloxifene, 1, is a selective estrogen receptor modulator (SERM) which is currently under clinical evaluation for the prevention and treatment of postmenopausal osteoporosis. In vivo structure- activity relationships and molecular
Conversion of the phytoestrogen coumestrol into a selective estrogen receptor modulator (SERM) by attachment of an amine-containing sidechain
Grese, Timothy A.,Cole, Harlan W.,Magee, David E.,Phillips, D. Lynn,Shetler, Pam K.,Short, Lorri L.,Glasebrook, Andrew L.,Bryant, Henry U.
, p. 2683 - 2686 (2007/10/03)
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.
