Structure-activity relationships of selective estrogen receptor modulators: modifications to the 2-arylbenzothiophene core of raloxifene

…, MJ Martin, K Matsumoto, LD Pennington…

Index: Grese, Timothy A.; Cho, Stephen; Finley, Don R.; Godfrey, Alexander G.; Jones, Charles D.; Lugar III, Charles W.; Martin, Michael J.; Matsumoto, Ken; Pennington, Lewis D.; Winter, Mark A.; Adrian, M. Dee; Cole, Harlan W.; Magee, David E.; Phillips, D. Lynn; Rowley, Ellen R.; Short, Lorri L.; Glasebrook, Andrew L.; Bryant, Henry U. Journal of Medicinal Chemistry, 1997 , vol. 40, # 2 p. 146 - 167

Full Text: HTML

Citation Number: 195

Abstract

The 2-arylbenzothiophene raloxifene, 1, is a selective estrogen receptor modulator which is currently under clinical evaluation for the prevention and treatment of postmenopausal osteoporosis. A series of raloxifene analogs which contain modifications to the 2- arylbenzothiophene core have been prepared and evaluated for the ability to bind to the estrogen receptor and inhibit MCF-7 breast cancer cell proliferation in vitro. Their ability to ...