Abstract
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.
Highlights
In clinical oncology, 2′-deoxy-2′-[18F]fluoro-D-glucose (18F-FDG), a glucose derivative, has been widely used in recent years for tumor imaging with positron emission tomography (PET)
F-FDG is a non-specific tracer for tumor imaging since glucose is highly utilized by many other cells, such as macrophages found in inflammatory lesions [1,2]
Molecules 2012, 17 thymidine (18F-FLT) [1,3,4,5] and its analog 18F-FMAU [8] have demonstrated their good imaging features. These tracers were labeled with either 11C or 18F, which are short half-life isotopes produced by a cyclotron, with complicated radiochemical synthesis and the lower radiochemical yield and high cost of PET examination, all of which limit their use as tracers in routine clinical studies
Summary
2′-deoxy-2′-[18F]fluoro-D-glucose (18F-FDG), a glucose derivative, has been widely used in recent years for tumor imaging with positron emission tomography (PET). F-FDG is a non-specific tracer for tumor imaging since glucose is highly utilized by many other cells, such as macrophages found in inflammatory lesions [1,2]. Molecules 2012, 17 thymidine (18F-FLT) [1,3,4,5] and its analog 18F-FMAU [8] have demonstrated their good imaging features These tracers were labeled with either 11C or 18F, which are short half-life isotopes produced by a cyclotron, with complicated radiochemical synthesis and the lower radiochemical yield and high cost of PET examination, all of which limit their use as tracers in routine clinical studies. Two novel 99mTc-labeled thymidine derivatives were prepared and reported, i.e., 99mTc-TMHEA and 99mTc-TMHHA (Figure 1) Their in vitro stability and in vivo biodistribution were studied
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