Timothy Alan Grese

TL;DR: Structural differences between raloxifene and tamoxifen may influence the conformations of their respective receptor/ligand complexes, thereby affecting which estrogen-responsive genes are modulated in various tissues, indicating that differences in tissue selective actions among benzothiophene and triarylethylene estrogen receptor modulators can be ascribed to discrete ligand conformations.

TL;DR: It is demonstrated that the 6-hydroxy and, to a lesser extent, the 4'-hydroxy substituents of raloxifene are important for receptor binding and in vitro activity, and small, highly electronegative 4'-substituents such as hydroxy, fluoro, and chloro are preferred both in vitro and in vivo.

TL;DR: It is demonstrated that one of these compounds, LY357489,4, is among the most potent SERMs described to date with in vivo efficacy on bone and cholesterol metabolism in OVX rats at doses as low as 0.01 mg/kg/d.

TL;DR: A review of selective estrogen receptor modulators can be found in this article, with an emphasis on structure activity relationships and on their effects in non-traditional target tissues, such as the skeleton, the cardiovascular system, and the central nervous system.