Development of Bifunctional Chelates Bearing Hydroxamate
Arms for Highly Efficient <sup>64</sup>Cu Radiolabeling
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Abstract
Convenient approaches for the synthesis
of DOTHA<sub>2</sub> and
NOTHA<sub>2</sub>, two cyclic bifunctional chelates (BFCs) bearing
hydroxamate arms, have been developed. These novel BFCs coordinate <sup>64</sup>Cu with fast kinetics at room temperature in a wide range
of concentrations and pH. The corresponding radiochemical complexes
showed high stability, low residual activity in various tissues, and
fast clearance in normal mice. The ability to conjugate DOTHA<sub>2</sub> to both a small peptide and a large protein is also reported
