Considerable research efforts have been directed towards developing the adequate ligand for use in radioimmunotherapy (RIT), an antibody targeted cancer therapeutic technique. The success of clinical applications of RIT heavily depends on the performance of the ligand used for effectively sequestering a radionuclide after being conjugated to an antibody. The New types of ligands possessing both a macrocyclic cavity and an acyclic pendant binding group have been designed based on the hypothesis that the bimodal binding using both a macrocyclic cavity and an acyclic pendant donor groups may provide enhanced kinetics in metal complexation while maintaining a high level of complex stability. We herein report the novel bimodal ligands, NETA, NE3TA, and DEPA that may have broad applicability for use in RIT. The efficient and short synthetic procedure to the new ligands will be presented.