Practical and scalable synthesis of amino acids and their use as precursor molecules of the bifuntional ligands for cancer therapy and imaging

CHED 273

Hyunbeom Lee, chong@iit.edu and Hyun-Soon Chong. Chemistry Division, Biological, Chemical, and Physical Sciences Department, Illinois Institute of Technology, 3101 S. Dearborn St., LS 182, Chicago, IL 60616
The development of the adequate synthetic bifunctional chelates is a critical step for targeted magnetic resonance imaging (MRI) and an antibody-targeted cancer therapeutic technique, radioimmunotherapy (RIT). We previously reported the synthesis and biological evaluation of the structually new bifunctional ligand, C-NETA possessing both a macrocyclic cavity and an acyclic pendant binding group for use in MRI and RIT. We have developed a practical, efficient, and scalable synthetic route to amino acids having a linker for conjugation to antibody, a tumor targeting moiety. The amino acids are further converted to precursor molecules for bifunctional ligands. We will present the efficient synthetic route to amino acids and the progress towards the synthesis of new bifunctional ligand, 5p-C-NETA for targeted cancer therapy and imaging.