Syntheses and biological activities of novel 2-methoxyestradiol analogs 2-fluoroethoxyestradiol and 2-fluoropropanoxyestradiol and a radiosynthesis of 2-18Ffluoroethoxyestradiol for positron emission tomography

摘要

Introduction2-Methoxyestradiol (2ME2) is an endogenous metabolite of the human hormone, estrogen, which has been shown to possess anti-tumor activity. 2-Fluoroethoxyestradiol (2FEE2) and 2-fluoropropanoxyestradiol (2FPE2), novel analogs of 2-methoxyestradiol, were designed and synthesized to be utilized as F-18 radiotracers for positron emission tomography (PET), with which the bio-distribution and intratumoral accumulations of 2ME2 could be measured in vivo for potential translation to human use.