151869-60-2Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of novel estradiol-bisphosphonate conjugates as bone-specific estrogens
Morioka, Masahiko,Kamizono, Akihito,Takikawa, Hirosato,Mori, Akihisa,Ueno, Hiroaki,Kadowaki, Shu-ichiro,Nakao, Yoshihide,Kato, Kuniki,Umezawa, Kazuo
experimental part, p. 1143 - 1148 (2010/04/24)
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 (E2-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 E2-BPs was essential for the absorption and specificity of the conjugates.
