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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 
 
 

KIH-802: 2-nitroimidazole-1-acetohydroxamate as a hypoxic cell radiosensitizer.

We have identified potassium 2-nitroimidazole-1-acetohydroxamate (KIH-802) as a hypoxic cell radiosensitizer potentially superior to Miso. The water-soluble acetohydroxamates of 2-nitroimidazole (KIH-802; free acid 801) and 4-nitroimidazole (KIH-852) were designed, synthesized, and evaluated by in vitro and in vivo screening against EMT6 cells. Enhancement ratios of KIH-802 and 801 were 1.92 and 1.68, respectively, compared with 1.58 for MISO all at 1 mM. These acetohydroxamates are also expected to be more effective in vitro than SR-2508 based on our previous experiments. In vivo ERs of KIH-802, 801, and 852 were 1.75, 1.50, and 1.35, respectively, compared with 1.57 for MISO all at the same dose of 200 mg/kg. The data clearly show that the addition of an acetohydroxamic acid moiety to the 2-nitroimidazole skeleton can enhance radiosensitizing ability.[1]

References

  1. KIH-802: 2-nitroimidazole-1-acetohydroxamate as a hypoxic cell radiosensitizer. Hori, H., Murayama, C., Mori, T., Shibamoto, Y., Abe, M., Onoyama, Y., Inayama, S. Int. J. Radiat. Oncol. Biol. Phys. (1989) [Pubmed]
 
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