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 


Vol. 34,  No. 12, pp. 3654-3658, Dec.  2013
10.5012/bkcs.2013.34.12.3654


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  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 R1 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 ε* 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.

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  Cite this article

[IEEE Style]

K. S. Nam, K. Jung, Y. Chang, T. Kim, "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," Bulletin of the Korean Chemical Society, vol. 34, no. 12, pp. 3654-3658, 2013. DOI: 10.5012/bkcs.2013.34.12.3654.

[ACM Style]

Ki Soo Nam, Ki-Hye Jung, Yongmin Chang, and Tae-Jeong Kim. 2013. 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. Bulletin of the Korean Chemical Society, 34, 12, (2013), 3654-3658. DOI: 10.5012/bkcs.2013.34.12.3654.

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ISSN(Print) 0253-2964
ISSN(Online) 1229-5949