The 2-[(3-carboxy-1-oxopropyl) amino]-2-deoxy-D-glucose (CPADG) was synthesized and radiolabeled with (TcO4)-Tc-99m to obtain the Tc-99m-CPADG complex in high yield. It was stable over 6 h in saline at room temperature and in serum at 37 degrees C. The partition coefficient and electrophoresis results indicated that the complex was hydrophilic and cationic. In vitro cell studies showed there was an increase in the uptake of Tc-99m-CPADG as a function of incubation time and Tc-99m-CPADG was possibly transported via the glucose transporters. The biodistribution of Tc-99m-CPADG in mice bearing S 180 tumor showed that the complex accumulated in the tumor with high uptake and good retention. The tumor/blood and tumor/muscle ratios increased with time and reached 1.91 and 5.05 at 4 h post-injection. Single photon emission computed tomography (SPECT) image studies showed there was an obvious accumulation in tumor sites, suggesting Tc-99m-CPADG would be a promising candidate for tumor imaging. (C) 2014 Elsevier Ltd. All rights reserved.
基金：
National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21171024, 81101069]; Beijing Natural Science FoundationBeijing Natural Science Foundation [7112035]; Fundamental Research Funds for the Central UniversitiesFundamental Research Funds for the Central Universities [105566]; Beijing Nova ProgramBeijing Municipal Science & Technology Commission [xxhz201306]
第一作者单位：[1]Beijing Normal Univ, Coll Chem, Minist Educ, Key Lab Radiopharmaceut, Beijing 100875, Peoples R China
通讯作者：
推荐引用方式(GB/T 7714)：
Wang Yue,Zhu Jingjing,Song Xiaoqing,et al.Synthesis and evaluation of Tc-99m-2-[(3-carboxy-1-oxopropyl)amino]-2-deoxy-D-glucose as a potential tumor imaging agent[J].BIOORGANIC & MEDICINAL CHEMISTRY LETTERS.2014,24(16):3882-3885.doi:10.1016/j.bmcl.2014.06.051.
APA：
Wang, Yue,Zhu, Jingjing,Song, Xiaoqing,Wang, Xuebin,Yang, Jigang&Zhang, Junbo.(2014).Synthesis and evaluation of Tc-99m-2-[(3-carboxy-1-oxopropyl)amino]-2-deoxy-D-glucose as a potential tumor imaging agent.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,24,(16)
MLA：
Wang, Yue,et al."Synthesis and evaluation of Tc-99m-2-[(3-carboxy-1-oxopropyl)amino]-2-deoxy-D-glucose as a potential tumor imaging agent".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 24..16(2014):3882-3885
