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 language | English |
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Pages (from-to) | 3654-3658 |
Number of pages | 5 |
Journal | Bulletin of the Korean Chemical Society |
Volume | 34 |
Issue number | 12 |
DOIs | |
State | Published - 20 Dec 2013 |
Keywords
- Aniline benzothiazole
- DO3A
- Gadolinium
- MRI
- Tumor-targeting