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

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 T hepatobiliary magnetic resonance imaging (MRI) contrast agent. The new macrocyclic liver agent...

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Veröffentlicht in:Journal of medicinal chemistry 2017-06, Vol.60 (12), p.4861-4868
Hauptverfasser: Baek, Ah Rum, Kim, Hee-Kyung, Park, Subin, Lee, Gang Ho, Kang, Hyo Jeung, Jung, Jae-Chang, Park, Joon-Suk, Ryeom, Hun-Kyu, Kim, Tae-Jeong, Chang, Yongmin
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Sprache:eng
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Zusammenfassung: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 T hepatobiliary magnetic resonance imaging (MRI) contrast agent. The new macrocyclic liver agent shows high chelation stability and high r 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.
ISSN:0022-2623
1520-4804
DOI:10.1021/acs.jmedchem.7b00060