1 research outputs found
Triazole Appending Agent (TAAG): A New Synthon for Preparing Iodine-Based Molecular Imaging and Radiotherapy Agents
A new prosthetic group referred to as the triazole appending
agent (TAAG) was developed as a means to prepare targeted radioiodine-based
molecular imaging and therapy agents. Tributyltin-TAAG and the fluorous
analogue were synthesized in high yield using simple click chemistry
and the products labeled in greater than 95% RCY with <sup>123</sup>I. A TAAG derivative of an inhibitor of prostate-specific membrane
antigen was prepared and radiolabeled with <sup>123</sup>I in 85%
yield where biodistribution studies in LNCap prostate cancer tumor
models showed rapid clearance of the agent from nontarget tissues
and tumor accumulation of 20% injected dose g<sup>–1</sup> at
1 h. The results presented demonstrate that the TAAG group promotes
minimal nonspecific binding and that labeled conjugates can achieve
high tumor uptake and exquisite target-to-nontarget ratios