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

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• 作者：Alla Darwish ; Megan Blacker ; Nancy Janzen ; Stephanie M. Rathmann ; Shannon Czorny ; Shawn M. Hillier ; John L. Joyal ; John W. Babich ; John F. Valliant
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2012
• 出版时间：April 12, 2012
• 年：2012
• 卷：3
• 期：4
• 页码：313-316
• 全文大小：215K
• 年卷期：v.3,no.4(April 12, 2012)
• ISSN：1948-5875

文摘

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 ¹²³I. A TAAG derivative of an inhibitor of prostate-specific membrane antigen was prepared and radiolabeled with ¹²³I 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^鈥? 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.

Keywords:

imaging; iodine; radiochemistry; radiopharmaceuticals; SPECT