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Non-cross-bridged tetraazamacrocyclic chelator for stable (64)cu-based radiopharmaceuticals.

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 (64)Cu ions and showed rapid clearance from the body to emerge as a potential efficient bifunctional chelator.

SUBMITTER: Dale AV

PROVIDER: S-EPMC4027512 | biostudies-literature | 2013 Oct

REPOSITORIES: biostudies-literature

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Non-cross-bridged tetraazamacrocyclic chelator for stable (64)cu-based radiopharmaceuticals.

Dale Ajit V AV Pandya Darpan N DN Kim Jung Young JY Lee Hochun H Ha Yeong Su YS Bhatt Nikunj N Kim Jonghee J Seo Jeong Ju JJ Lee Woonghee W Kim Sung Hong SH Yoon Young-Ran YR An Gwang Il GI Yoo Jeongsoo J

ACS medicinal chemistry letters 20130725 10

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 (64)Cu ions and showed rapid clearance from the body to emerge as a potential efficient bifunctional chelator. ...[more]

PMID: 24900586

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