Gadolinium complex of 1,4,7,10-tetraazacyclododecane-1,4,7-trisacetic acid (do3a) conjugate of [(p-aniline benzothiazole)methyl]pyridine as a tumor-targeting mri contrast agent

Ki Soo Nam, Ki Hye Jung, Yongmin Chang, Tae Jeong Kim

Research output: Contribution to journalArticlepeer-review

3 Scopus citations

Abstract

The synthesis of a DO3A conjugate of [(p-aniline benzothiazole)methyl] pyridine (L2H3) and its gadolinium complex of the type [Gd(L2)(H2O)] (GdL2) is described. The R 1 relaxivity (= 4.50 mM-1sec-1) and kinetic inertness of GdL2 compares well with those of structurally analogous Dotarem® (R1 = 3.70 mM-1sec-1), a typical extracellular (ECF) MRI contrast agent (CA). Yet, by comparison with Dotarem®, GdL2 exhibits noncovalent interactions with human serum albumin (HSA) as evidenced by the e* titration curve along with in vivo MR signal enhancement in both aorta and heart. Liver-specific nature of GdL2 is also observed as excretion is made through gallbladder. Most notably, GdL2 further demonstrates specificity toward the MDAMB-231 breast cancer.

Original languageEnglish
Pages (from-to)3654-3658
Number of pages5
JournalBulletin of the Korean Chemical Society
Volume34
Issue number12
DOIs
StatePublished - 20 Dec 2013

Keywords

  • Aniline benzothiazole
  • DO3A
  • Gadolinium
  • MRI
  • Tumor-targeting

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