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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 BaekHee-Kyung KimSubin ParkGang Ho LeeHyo Jeung KangJae-Chang JungJoon-Suk ParkHun-Kyu RyeomTae-Jeong KimYongmin Chang
Published in: Journal of medicinal chemistry (2017)
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.
Keyphrases
  • contrast enhanced
  • magnetic resonance imaging
  • magnetic resonance
  • computed tomography
  • diffusion weighted imaging
  • mass spectrometry
  • photodynamic therapy
  • drug administration