David Lynn Phillips

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: 4c is identified as a novel SERM with greater potency to antagonize estrogen in uterine tissue and in human mammary cancer cells compared to raloxifene, tamoxifen or ICI-182,780.

TL;DR: Representative non-steroidal estrogens, from common environmental sources such as plants, pesticides, surfactants, plastics, and animal health products, demonstrated an ability to lower serum cholesterol and prevent bone loss in an estrogen-dependent animal model, the ovariectomized rat.

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: The present findings support the classification of raloxifene as a selective estrogen receptor modulator in ovariectomized rats and mediated primarily via partial agonist effects at estrogen receptors.