Structure-activity relationships of SERMs optimized for uterine antagonism and ovarian safety.
Basic Information
ID: ALA1145362
Journal: Bioorg Med Chem Lett
Title: Structure-activity relationships of SERMs optimized for uterine antagonism and ovarian safety.
Authors: Richardson TI, Frank SA, Wang M, Clarke CA, Jones SA, Ying BP, Kohlman DT, Wallace OB, Shepherd TA, Dally RD, Palkowitz AD, Geiser AG, Bryant HU, Henck JW, Cohen IR, Rudmann DG, McCann DJ, Coutant DE, Oldham SW, Hummel CW, Fong KC, Hinklin R, Lewis G, Tian H, Dodge JA.
Abstract: Structure-activity relationship studies are described, which led to the discovery of novel selective estrogen receptor modulators (SERMs) for the potential treatment of uterine fibroids. The SAR studies focused on limiting brain exposure and were guided by computational properties. Compounds with limited impact on the HPO axis were selected using serum estrogen levels as a biomarker for ovarian stimulation.
CiteXplore: 17482463
DOI: 10.1016/j.bmcl.2007.04.044
Patent ID: ┄