Document Report Card
Basic Information
ID: ALA1156856
Journal: Bioorg Med Chem
Title: Design, synthesis, and biological evaluation of novel estradiol-bisphosphonate conjugates as bone-specific estrogens.
Authors: Morioka M, Kamizono A, Takikawa H, Mori A, Ueno H, Kadowaki S, Nakao Y, Kato K, Umezawa K.
Abstract: Bone deficiency causes osteoporosis and often decreases quality of life in patients with rheumatoid arthritis. Estrogens are known to protect elderly women from bone loss. Synthesis of new estradiol-bisphosphonate conjugates (E(2)-BPs) was accomplished and their in vivo activity as bone-specific estrogens were examined. Among them, MCC-565 showed selective estrogenic activity in bones; but it showed little estrogenic activity in the uterus. We also found that the linker moiety in E(2)-BPs was essential for the absorption and specificity of the conjugates.
CiteXplore: 20071185