Non-cross-bridged tetraazamacrocyclic chelator for stable 64Cu-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 ⁶⁴Cu-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

Department of Energy and Science and Engineering

Research output: Contribution to journal › Article › peer-review

21 Scopus citations

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.

Original language	English
Pages (from-to)	927-931
Number of pages	5
Journal	ACS Medicinal Chemistry Letters
Volume	4
Issue number	10
DOIs	https://doi.org/10.1021/ml400142s
State	Published - 10 Oct 2013

Keywords

Bifunctional chelator
copper complex
imaging agent
radiopharmaceutical

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10.1021/ml400142s

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title = "Non-cross-bridged tetraazamacrocyclic chelator for stable 64Cu-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 64Cu ions and showed rapid clearance from the body to emerge as a potential efficient bifunctional chelator.",

keywords = "Bifunctional chelator, copper complex, imaging agent, radiopharmaceutical",

author = "Dale, \{Ajit V.\} and Pandya, \{Darpan N.\} and Kim, \{Jung Young\} and Hochun Lee and Ha, \{Yeong Su\} and Nikunj Bhatt and Jonghee Kim and Seo, \{Jeong Ju\} and Woonghee Lee and Kim, \{Sung Hong\} and Yoon, \{Young Ran\} and An, \{Gwang Il\} and Jeongsoo Yoo",

year = "2013",

month = oct,

day = "10",

doi = "10.1021/ml400142s",

language = "English",

volume = "4",

pages = "927--931",

journal = "ACS Medicinal Chemistry Letters",

issn = "1948-5875",

publisher = "American Chemical Society",

number = "10",

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TY - JOUR

T1 - Non-cross-bridged tetraazamacrocyclic chelator for stable 64Cu-based radiopharmaceuticals

AU - Dale, Ajit V.

AU - Pandya, Darpan N.

AU - Kim, Jung Young

AU - Lee, Hochun

AU - Ha, Yeong Su

AU - Bhatt, Nikunj

AU - Kim, Jonghee

AU - Seo, Jeong Ju

AU - Lee, Woonghee

AU - Kim, Sung Hong

AU - Yoon, Young Ran

AU - An, Gwang Il

AU - Yoo, Jeongsoo

PY - 2013/10/10

Y1 - 2013/10/10

N2 - 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.

AB - 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.

KW - Bifunctional chelator

KW - copper complex

KW - imaging agent

KW - radiopharmaceutical

UR - https://www.scopus.com/pages/publications/84885462532

U2 - 10.1021/ml400142s

DO - 10.1021/ml400142s

M3 - Article

AN - SCOPUS:84885462532

SN - 1948-5875

VL - 4

SP - 927

EP - 931

JO - ACS Medicinal Chemistry Letters

JF - ACS Medicinal Chemistry Letters

IS - 10

ER -

Non-cross-bridged tetraazamacrocyclic chelator for stable ⁶⁴Cu-based radiopharmaceuticals

Abstract

Keywords

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