Synthesis and pharmacology of 2-alkyl raloxifene analogs

…, S Cho, HU Bryant, HW Cole, AL Glasebrook…

Index: Grese, Timothy A.; Cho, Stephen; Bryant, Henry U.; Cole, Harlan W.; Glasebrook, Andrew L.; et al. Bioorg. Med. Chem. Lett., 1996 , vol. 6, # 2 p. 201 - 206

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Citation Number: 12

Abstract

A series of 2-alkyl and 2-cycloalkyl raloxifene analogs have been prepared and evaluated in both in vitro and in vivo models of estrogen/antiestrogen activity. In particular, the 2- cyclohexyl analogs show promise as potent selective estrogen-receptor modulators (SERMs).

~78%

Structure-activity relationships of selective estrogen recep...

[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]