Preparation and preliminary biological evaluation of novel (99m)Tc-labelled thymidine analogs as tumor imaging agents.
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 (99m)Tc in high labeling yields. The in vitro stability and in vivo biodistribution of (99m)Tc-TMHEA and (99m)Tc-TMHHA were investigated and compared. The biodistribution studies indicate that the radiotracer (99m)Tc-TMHEA displays selective tumor uptake, suggesting it is a potential tumor imaging agent.
Key Laboratory of Nuclear Medicine, Ministry of Health-Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China. luchunxiong@yahoo.com.cn
Chunxiong
C
Lu
Quanfu
Q
Jiang
Cheng
C
Tan
Jie
J
Tang
Jiankang
J
Zhang
D020003:1-Octanol / Q000737:chemistry; D000818:Animals; D003952:Diagnostic Imaging; D051379:Mice; D008813:Mice, Inbred ICR; D009369:Neoplasms / Q000175:diagnosis*; D013194:Staining and Labeling; D013667:Technetium / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D013936:Thymidine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D014018:Tissue Distribution; D018675:Toxicity Tests; D014867:Water / Q000737:chemistry
D014867:Water; D013667:Technetium; D020003:1-Octanol; D013936:Thymidine