Hee-Kyung Kim1,
Ki-Hye Jung2, Min-Kyoung Kang1, Ji-Ae Park3,
Eun-Young Jeon4, Seung-Tae Woo5, Joo-Hyun Kim5,
Tae-Jeong Kim2, Yongmin Chang1, 6
1Medical
& Biological Engineering, Kyungpook National University, Daegu, Korea; 2Applied
Chemistry, Kyungpook National University, Daegu, Korea; 3Molecular
Imaging Research Center, Korea Institute of Radiological & Medical
Science, Seoul, Korea; 4The Advanced Medical Technology Cluster
for Diagnosis & Prediction, Kyungpook National University, Daegu, Korea; 5Bayer
Healthcare, Medical Care, Seoul, Korea; 6Diagnostic Radiology and
Molecular Medicine, Kyungpook National University, Daegu, Korea
DO3A-benzothiazole conjugates have been prepared as a new family of multifunctional MRI/optical imaging probes with concomitant antitumor activity as well as tumor-specificity. Its R1 relaxivity is 3.84 mM-1sec-1, almost the same values as that of structurally related Dotarem&[reg]. The pattern of in vivo MRI enhacement compares well with those of liver-specific MRI CAs. More characteristically, it is to be noted that excretion is made via bile duct, confirming hepatobiliary uptake. T1-weighted MR images of MCF-7 cells incubated with Gd-DO3A-BT, revealing the tumor-specificity of the present series. In addition, antitumor activity of the present system represented as GI50 and TGI values.
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