| abstract |
Macrocyclic chelators (I) for the chelation of alpha-emitting radiometal ions, such as actinium-225, are provided. Also provided are radiometal complexes containing an alpha-emitting radiometal ion bound to the macrocyclic chelator via coordinate bonding, and radioimmunoconjugates containing the radiometal complexes covalently bound to a targeted ligand, such as an antibody or antigen-binding fragment of East. Radioimmunoconjugates can be produced by chemical click reactions. Methods of using the radiocomplexes and radioimmunoconjugates to selectively target neoplastic cells for radiation therapy and to treat neoplastic diseases and disorders are also described. |