American Chemical Society
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Non-Cross-Bridged Tetraazamacrocyclic Chelator for Stable 64Cu-Based Radiopharmaceuticals

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journal contribution
posted on 2016-02-18, 16:41 authored by Ajit V. Dale, Darpan N. Pandya, Jung Young Kim, Hochun Lee, Yeong Su Ha, Nikunj Bhatt, Jonghee Kim, Jeong Ju Seo, Woonghee Lee, Sung Hong Kim, Young-Ran Yoon, Gwang Il An, Jeongsoo Yoo
N-mono/dimethylated TE2A tetraazamacrocycles (MM-TE2A and DM-TE2A) were synthesized in high yields. Both Cu-MM/DM-TE2A complexes showed increased kinetic stability compared to that of Cu-TE2A, whereas Cu-DM-TE2A showed even higher in vitro stability than that of Cu-ECB-TE2A. MM-TE2A and DM-TE2A were quantitatively radiolabeled with 64Cu ions and showed rapid clearance from the body to emerge as a potential efficient bifunctional chelator.