Detection of carcinogenic cells is essential for the successful treatment of cancer. For cancers such as breast, melanoma, and prostate, early detection (during stage one) informs crucial intervention. Positron Emission Tomography (PET) has established itself as a leading method of detection for these cancers, where the design of theranostic agents capable of both imaging and treatment are highly desirable. 64Cu ( t1/2 = 12.7 h, β+ = 653 keV) and 67Cu (t1/2 = 61.9 h, β- =141 keV) are theranostic pairs with decay characteristics suitable for PET and targeted radiotherapy, but require rationally designed bifunctional chelates that can form inert Cu complexes and can be easily conjugated to specific cell targeting agents. Recently, we’ve discovered a new class of cyclen-derived polyaminocarboxylates that feature a spirocyclic ammonium group which can form thermodynamically stable complexes with copper-64 and display high stability in blood plasma. In this poster, we will discuss our recent progress in the synthesis and characterization of novel derivatives which are amenable to conjugation with small molecule targeting agents that will ultimately enable theranostic applications for early-stage cancer detection and treatment.

Progress towards incorporating conjugatable linkers in a novel azamacrocycle designed to chelate 64Cu

ACS Spring 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.