UIC-2019-079 – Novel, Bifunctional Chelating Agent

Leading chemistry research labs at UIC, the Wardrop and Miller labs, present a novel 4-C functionalized- 1,2-trans-cyclohexyldiamine chelating agent. The primary embodiment would be 4-C functionalized CyDTPA, meaning the conjugation site is distal to the coordination sphere. 4-C functionalization minimizes interactions between the conjugate and the coordination sphere. Moreover, the synthetic pathway yields a single diastereomer, eliminating the need for extensive purification. Placement of the conjugation site proximal to the coordination sphere and diastereomer impurities lead to differential in vivo stability, which can be disastrous for clinical applications of RIT. All RIT requires a bifunctional chelating agent to both bind the radionuclide and the targeting compounds. Chelating agent synthesis is strictly bound by competing design objectives such as stability and rapid complex formation. Due to these limitations, there has been little advancement in the design of bifunctional chelating agents suitable for RIT. Nelson Grihalde grihalde@otm.uic.edu 312-996-4129