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10.1021/ml300003v

http://scihub22266oqcxt.onion/10.1021/ml300003v
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suck abstract from ncbi


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pmid24900470
      ACS+Med+Chem+Lett 2012 ; 3 (4 ): 313-6
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  • Triazole Appending Agent (TAAG): A New Synthon for Preparing Iodine-Based Molecular Imaging and Radiotherapy Agents #MMPMID24900470
  • Darwish A ; Blacker M ; Janzen N ; Rathmann SM ; Czorny S ; Hillier SM ; Joyal JL ; Babich JW ; Valliant JF
  • ACS Med Chem Lett 2012[Apr]; 3 (4 ): 313-6 PMID24900470 show ga
  • 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.
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