Preparation and Preliminary Biological Evaluation of Novel <sup>99m</sup>Tc-Labelled Thymidine Analogs as Tumor Imaging Agents

• Main Authors: Jiankang Zhang, Cheng Tan, Chunxiong Lu, Quanfu Jiang, Jie Tang
• Format: Article
• Language: English
• Published: MDPI AG 2012-07-01
• Series: Molecules
• Subjects: thymidine derivative; <sup>99m</sup>Tc-labelled; biodistribution; tumor imaging
• Online Access: http://www.mdpi.com/1420-3049/17/7/8518

Two kinds of novel thymidine derivatives, <em>N</em>-thymidine-yl-<em>N′</em>-methyl-<em>N′</em>-{<em>N′′</em>-[2-sulfanyl-(ethylamino)acetyl]-2-aminoethylsulfanyl-1-hexanamide}-ethanediamine (TMHEA) and <em>N</em>-thymidine-yl-<em>N′</em>-methyl-<em>N′</em>-{<em>N′′</em>-[2-sulfanyl-(ethylamino)acetyl]-2-aminoethylsulfanyl-1-hexanamide}-hexanediamine (TMHHA) were prepared and successfully labeled with <sup>99m</sup>Tc in high labeling yields. The <em>in vitro </em>stability and <em>in vivo</em> biodistribution of <sup>99m</sup>Tc-TMHEA and <sup>99m</sup>Tc-TMHHA were investigated and compared. The biodistribution studies indicate that the radiotracer <sup>99m</sup>Tc-TMHEA displays selective tumor uptake, suggesting it is a potential tumor imaging agent.