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

Dale, Ajit V.; Pandya, Darpan N.; Kim, Jung Young; Lee, Hochun; Ha, Yeong
Su; Bhatt, Nikunj; Kim, Jonghee; Seo, Jeong Ju; Lee, Woonghee; Kim, Sung Hong; Yoon, Young-Ran; An, Gwang Il; Yoo, Jeongsoo

doi:10.1021/ml400142s.s001

ml400142s_si_001.pdf (2.05 MB)

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

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.