Synthesis and in vitro evaluation of three 99mTc-labeled hydroxamamide-based ligands as markers for hypoxic cells.
Three new hydroxamamide derivatives with different lipophilicity, N'-hydroxy-N-methyl-3-(4-nitro-1H-imidazol-1-yl)propanamidine, N-butyl-N'-hydroxy-3-(4-nitro-1H-imidazol-1-yl)propanamidine, and N'-hydroxy-3-(4-nitro-1H-imidazol-1-yl)-N-octadecylpropanamidine were easily synthesized and labeled with technetium-99m as markers for hypoxic cells. The results of in vitro experiment indicate that the accumulation of three (99m)Tc-complexes steadily increases with time in hypoxic cells, but fluctuates with time and has no fixed trend in aerobic cells; the complex with higher lipophilicity shows more uptake in cells; and the effect of lipophilicity of the (99m)Tc-complexes on the hypoxic/aerobic difference can be neglected.
Chu
Taiwei
T
Beijing National Laboratory for Molecular Sciences, Department of Applied Chemistry, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China. twchu@pku.edu.cn
Xu
Hong
H
Yang
Zhi
Z
Wang
Xiangyun
X
D000577:Amides / Q000138:chemical synthesis* / Q000494:pharmacology*; D015687:Cell Hypoxia; D004353:Drug Evaluation, Preclinical; D004590:Electrophoresis, Paper; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*
D000577:Amides; D008024:Ligands; D015609:Organotechnetium Compounds