Gadolinium Complex of 1,4,7,10-Tetraazacyclododecane-1,4,7-Trisacetic Acid (DO3A)-Ethoxybenzyl (EOB) Conjugate as a New Macrocyclic Hepatobiliary MRI Contrast Agent

Ah Rum Baek; Hee Kyung Kim; Subin Park; Gang Ho Lee; Hyo Jeung Kang; Jae Chang Jung; Joon Suk Park; Hun Kyu Ryeom; Tae Jeong Kim; Yongmin Chang

doi:10.1021/acs.jmedchem.7b00060

Gadolinium Complex of 1,4,7,10-Tetraazacyclododecane-1,4,7-Trisacetic Acid (DO3A)-Ethoxybenzyl (EOB) Conjugate as a New Macrocyclic Hepatobiliary MRI Contrast Agent

Ah Rum Baek, Hee Kyung Kim, Subin Park, Gang Ho Lee, Hyo Jeung Kang, Jae Chang Jung, Joon Suk Park, Hun Kyu Ryeom, Tae Jeong Kim, Yongmin Chang

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29 Scopus citations

Abstract

We report the synthesis of a macrocyclic Gd chelate based on a 1,4,7,10-Tetraazacyclododecane-1,4,7-Trisacetic acid (DO3A) coordinationn cage bearing an ethoxybenzyl (EOB) moiety and discuss its use as a T₁ hepatobiliary magnetic resonance imaging (MRI) contrast agent. The new macrocyclic liver agent shows high chelation stability and high r₁ relaxivity compared with linear-Type Gd chelates, which are the current clinically approved liver agents. Our macrocyclic, liver-specific Gd chelate was evaluated in vivo through biodistribution analysis and liver MRI, which demonstrated its high tumor detection sensitivity and suggested that the new Gd complex is a promising contrast agent for liver cancer imaging.

Original language	English
Pages (from-to)	4861-4868
Number of pages	8
Journal	Journal of Medicinal Chemistry
Volume	60
Issue number	12
DOIs	https://doi.org/10.1021/acs.jmedchem.7b00060
State	Published - 22 Jun 2017

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Baek, A. R., Kim, H. K., Park, S., Lee, G. H., Kang, H. J., Jung, J. C., Park, J. S., Ryeom, H. K., Kim, T. J., & Chang, Y. (2017). Gadolinium Complex of 1,4,7,10-Tetraazacyclododecane-1,4,7-Trisacetic Acid (DO3A)-Ethoxybenzyl (EOB) Conjugate as a New Macrocyclic Hepatobiliary MRI Contrast Agent. Journal of Medicinal Chemistry, 60(12), 4861-4868. https://doi.org/10.1021/acs.jmedchem.7b00060

@article{5c851ef8c21047fd9f9ba44b76c9d7ad,

title = "Gadolinium Complex of 1,4,7,10-Tetraazacyclododecane-1,4,7-Trisacetic Acid (DO3A)-Ethoxybenzyl (EOB) Conjugate as a New Macrocyclic Hepatobiliary MRI Contrast Agent",

abstract = "We report the synthesis of a macrocyclic Gd chelate based on a 1,4,7,10-Tetraazacyclododecane-1,4,7-Trisacetic acid (DO3A) coordinationn cage bearing an ethoxybenzyl (EOB) moiety and discuss its use as a T1 hepatobiliary magnetic resonance imaging (MRI) contrast agent. The new macrocyclic liver agent shows high chelation stability and high r1 relaxivity compared with linear-Type Gd chelates, which are the current clinically approved liver agents. Our macrocyclic, liver-specific Gd chelate was evaluated in vivo through biodistribution analysis and liver MRI, which demonstrated its high tumor detection sensitivity and suggested that the new Gd complex is a promising contrast agent for liver cancer imaging.",

author = "Baek, \{Ah Rum\} and Kim, \{Hee Kyung\} and Subin Park and Lee, \{Gang Ho\} and Kang, \{Hyo Jeung\} and Jung, \{Jae Chang\} and Park, \{Joon Suk\} and Ryeom, \{Hun Kyu\} and Kim, \{Tae Jeong\} and Yongmin Chang",

note = "Publisher Copyright: {\textcopyright} 2017 American Chemical Society.",

year = "2017",

month = jun,

day = "22",

doi = "10.1021/acs.jmedchem.7b00060",

language = "English",

volume = "60",

pages = "4861--4868",

journal = "Journal of Medicinal Chemistry",

issn = "0022-2623",

publisher = "American Chemical Society",

number = "12",

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Baek, AR, Kim, HK, Park, S, Lee, GH , Kang, HJ , Jung, JC, Park, JS, Ryeom, HK, Kim, TJ & Chang, Y 2017, 'Gadolinium Complex of 1,4,7,10-Tetraazacyclododecane-1,4,7-Trisacetic Acid (DO3A)-Ethoxybenzyl (EOB) Conjugate as a New Macrocyclic Hepatobiliary MRI Contrast Agent', Journal of Medicinal Chemistry, vol. 60, no. 12, pp. 4861-4868. https://doi.org/10.1021/acs.jmedchem.7b00060

TY - JOUR

T1 - Gadolinium Complex of 1,4,7,10-Tetraazacyclododecane-1,4,7-Trisacetic Acid (DO3A)-Ethoxybenzyl (EOB) Conjugate as a New Macrocyclic Hepatobiliary MRI Contrast Agent

AU - Baek, Ah Rum

AU - Kim, Hee Kyung

AU - Park, Subin

AU - Lee, Gang Ho

AU - Kang, Hyo Jeung

AU - Jung, Jae Chang

AU - Park, Joon Suk

AU - Ryeom, Hun Kyu

AU - Kim, Tae Jeong

AU - Chang, Yongmin

PY - 2017/6/22

Y1 - 2017/6/22

N2 - We report the synthesis of a macrocyclic Gd chelate based on a 1,4,7,10-Tetraazacyclododecane-1,4,7-Trisacetic acid (DO3A) coordinationn cage bearing an ethoxybenzyl (EOB) moiety and discuss its use as a T1 hepatobiliary magnetic resonance imaging (MRI) contrast agent. The new macrocyclic liver agent shows high chelation stability and high r1 relaxivity compared with linear-Type Gd chelates, which are the current clinically approved liver agents. Our macrocyclic, liver-specific Gd chelate was evaluated in vivo through biodistribution analysis and liver MRI, which demonstrated its high tumor detection sensitivity and suggested that the new Gd complex is a promising contrast agent for liver cancer imaging.

AB - We report the synthesis of a macrocyclic Gd chelate based on a 1,4,7,10-Tetraazacyclododecane-1,4,7-Trisacetic acid (DO3A) coordinationn cage bearing an ethoxybenzyl (EOB) moiety and discuss its use as a T1 hepatobiliary magnetic resonance imaging (MRI) contrast agent. The new macrocyclic liver agent shows high chelation stability and high r1 relaxivity compared with linear-Type Gd chelates, which are the current clinically approved liver agents. Our macrocyclic, liver-specific Gd chelate was evaluated in vivo through biodistribution analysis and liver MRI, which demonstrated its high tumor detection sensitivity and suggested that the new Gd complex is a promising contrast agent for liver cancer imaging.

UR - https://www.scopus.com/pages/publications/85021076360

U2 - 10.1021/acs.jmedchem.7b00060

DO - 10.1021/acs.jmedchem.7b00060

M3 - Article

C2 - 28530407

AN - SCOPUS:85021076360

SN - 0022-2623

VL - 60

SP - 4861

EP - 4868

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 12

ER -

Gadolinium Complex of 1,4,7,10-Tetraazacyclododecane-1,4,7-Trisacetic Acid (DO3A)-Ethoxybenzyl (EOB) Conjugate as a New Macrocyclic Hepatobiliary MRI Contrast Agent

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