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KIH-802, an acetohydroxamic acid derivative of 2-nitroimidazole, as a new potent hypoxic cell radiosensitizer: radiosensitizing activity, acute toxicity, and pharmacokinetics

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Summary

The radiosensitizing activity, acute toxicity, and pharmacokinetics of a new hypoxic cell radiosensitizer, potassium 2-nitroimidazole-1-acetohydroxamate (KIH-802), were compared with those of misonidazole (MISO) and etanidazole (SR-2508). The radiosensitizing activity of KIH-802 was slightly higher than that of MISO and SR-2508 in vitro and was similar to or slightly higher than that of MISO or SR-2508 in vivo. The acute toxicity of KIH-802 was slightly higher than that of MISO. The concentrations of KIH-802 in the brains and peripheral nerves of mice were as low as those of SR-2508 and lower than those of MISO.

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Authors and Affiliations

  1. Chest Disease Institute, Kyoto University, Japan

    Masaji Takahashi

  2. Department of Hydrocarbon Chemistry, Faculty of Engineering, Kyoto University, Japan

    Lin Zhou

  3. Department of Biological Science and Technology, Faculty of Engineering, Tokushima University, Japan

    Hitoshi Hori

  4. Pharmaceutical Institute, Faculty of Medicine, Keio University, Japan

    Hideko Nagasawa, Tetsuichi Shibata & Seiichi Inayama

  5. Department of Radiology, Faculty of Medicine, Kyoto University, 606, Sakyo-ku, Kyoto, Japan

    Keisuke Sasai, Yuta Shibamoto & Mitsuyuki Abe

Authors
  1. Keisuke Sasai
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  2. Yuta Shibamoto
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  3. Masaji Takahashi
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  4. Lin Zhou
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  5. Hitoshi Hori
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  6. Hideko Nagasawa
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  7. Tetsuichi Shibata
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  8. Seiichi Inayama
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  9. Mitsuyuki Abe
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Additional information

This work was supported in part by Grants-in-Aid from the Japanese Ministry of Education, Science and Culture (62010070, 63010070)

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Sasai, K., Shibamoto, Y., Takahashi, M. et al. KIH-802, an acetohydroxamic acid derivative of 2-nitroimidazole, as a new potent hypoxic cell radiosensitizer: radiosensitizing activity, acute toxicity, and pharmacokinetics. Cancer Chemother Pharmacol 26, 112–116 (1990). https://doi.org/10.1007/BF02897255

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  • DOI: https://doi.org/10.1007/BF02897255

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