Synthesis and characterization of chelating agents responsible for tumor imaging

摘要

Present study shows the Rationale behind the synthesis of chelating agents and their thermodynamic stability along with kinetic inertness of metal complex in vivo is the prerequisites for the successful application of bifunctional chelating agent- conjugate. Macrocyclic bifunctional chelating agents (BFCs) with their established stabilizing properties are in the forefront for radio-immuno applications. In this study macrocyclic BFCs with increase in rigidity for complex stability besides requisite flexibility for complexation along with variation in ring size and donor ligands group were aimed to study for radio-diagnostic applications. Aromatic chelating agents (5a, 5b and 5c) synthesized by following the synthetic route shown in scheme 1 and 2. Radio-complexation with 99mTc and conjugation with monoclonal antibody for tumor diagnosis was designed for final evaluation of efficiency of synthesized chelating agents.