211-ASTATINE CONTAINING RADIOTHERAPEUTICS FOR THE TREATMENT OF CANCER

摘要

Described herein is an alpha-emitting radionuclide, 211At, which has been incorporated into a selective sigma-2 ligand moiety to provide cytotoxic capabilities to a chemical compound. As described herein, a compound of formula (I), wherein R1-R4, m, and n are defined herein, was prepared and utilized in in vitro and in vivo tumor targeting of alpha-emitting sigma-2 ligand in a breast cancer model. In one embodiment, the compound is 5-(211At)-N-(4-(6,7-dimethoxy-3,4- dihydroisoquinolin-2(lH)-yl)butyl)-2,3-dimethoxybenzamide.