DGIST Scholar: Non-Cross-Bridged Tetraazamacrocyclic Chelator for Stable Cu-64-Based Radiopharmaceuticals

Title: Non-Cross-Bridged Tetraazamacrocyclic Chelator for Stable Cu-64-Based Radiopharmaceuticals

Citation: Dale, Ajit V. (2013-10). Non-Cross-Bridged Tetraazamacrocyclic Chelator for Stable Cu-64-Based Radiopharmaceuticals. ACS Medicinal Chemistry Letters, 4(10), 927–931. doi: 10.1021/ml400142s

Author Keywords: Bifunctional chelator ; copper complex ; imaging agent ; radiopharmaceutical

Keywords: IN-VIVO STABILITY ; COMPLEXES ; COPPER(II) ; COPPER-64 ; CYCLAM ; BIODISTRIBUTION ; MACROCYCLES ; DERIVATIVES ; CHEMISTRY ; BEHAVIOR

Abstract: 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. © 2013 American Chemical Society.
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