Development of Bifunctional Chelates Bearing Hydroxamate Arms for Highly Efficient Cu-64 Radiolabeling

作者：Ait Mohand Samia; Denis Celine; Tremblay Genevieve; Paquette Michel; Guerin Brigitte^*

来源：Organic Letters, 2014, 16(17): 4512-4515.

DOI：10.1021/ol5020575

Convenient approaches for the synthesis of DOTHA(2) and NOTHA(2), two cyclic bifunctional chelates (BFCs) bearing hydroxamate arms, have been developed. These novel BFCs coordinate Cu-64 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(2) to both a small peptide and a large protein is also reported.

• 出版日期2014-9-5