Preparation and Preliminary Biological Evaluation of Novel 99mTc-Labelled Thymidine Analogs as Tumor Imaging Agents

Molecules

Chunxiong Lu¹  Quanfu Jiang¹  Cheng Tan¹  Jie Tang¹ 

[1] ¹Key Laboratory of Nuclear Medicine, Ministry of Health-Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China ²School of Chemical and Material Engineering, Jiangnan University, Wuxi 214122, China

关键词: thymidine derivative;    ^99mTc-labelled;    biodistribution;    tumor imaging;   

DOI  :  10.3390/molecules17078518

来源: mdpi

【 摘 要 】

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

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.