title: Synthesis and in vitro evaluation of three 99mTc-labeled hydroxamamide-based ligands as markers for hypoxic cells.
abstract: 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.
authors.affiliation: 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
authors.forename: Taiwei
authors.initials: T
authors.lastname: Chu
authors.forename: Hong
authors.initials: H
authors.lastname: Xu
authors.forename: Zhi
authors.initials: Z
authors.lastname: Yang
authors.forename: Xiangyun
authors.initials: X
authors.lastname: Wang
mesh_terms: 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*
chemical_list: D000577:Amides; D008024:Ligands; D015609:Organotechnetium Compounds