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 99mTc-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 99mTc-complexes on the hypoxic/aerobic difference can be neglected.

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