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

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

doi:10.1021/ml400142s

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

ACS Med Chem Lett. 2013 Jul 25;4(10):927-31. doi: 10.1021/ml400142s. eCollection 2013 Oct 10.

Authors

Affiliations

¹ Department of Molecular Medicine, Kyungpook National University School of Medicine , Daegu 700-422, South Korea.
² Molecular Imaging Research Centre, Korea Institute of Radiological and Medical Sciences , Seoul 139-706, South Korea.
³ Department of Energy Systems Engineering, Daegu Gyeongbuk Institute of Science & Technology, Daegu 711-873, South Korea.
⁴ Department of Biomedical Science and Clinical Trial Center, Kyungpook National University Graduates School and Hospital , Daegu, South Korea.
⁵ Analysis Research Division, Daegu Center, Korea Basic Science Institute , Daegu 702-701, South Korea.

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.

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