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 Medicine

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",

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day = "10",

doi = "10.1021/ml400142s",

language = "English",

volume = "4",

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journal = "ACS Medicinal Chemistry Letters",

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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

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U2 - 10.1021/ml400142s

DO - 10.1021/ml400142s

M3 - Article

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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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