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Abstract #1879

DO3A-Benzothiazole Conjugates for Use as Gd-Based Theragnostic Agents

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.