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Triazole Appending Agent (TAAG): A New Synthon for Preparing Iodine-Based Molecular Imaging and Radiotherapy Agents.

Autor(es): Darwish, Alla; Blacker, Megan; Janzen, Nancy; Rathmann, Stephanie M; Czorny, Shannon; Hillier, Shawn M; Joyal, John L; Babich, John W; Valliant, John F
Fonte: ACS Med Chem Lett;3(4): 313-6, 2012 Apr 12.
Artigo [ PMID: 24900470 ] Idioma(s): Inglês
Publicação: Artigo de Revista
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 (123)I. A TAAG derivative of an inhibitor of prostate-specific membrane antigen was prepared and radiolabeled with (123)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(-1) 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.