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Antitumor activity of MST-16, a novel derivative of bis(2,6-dioxopiperazine), in murine tumor models

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Summary

We studied the antitumor activity of newly synthesized bis(1-acyloxymethyl) derivatives of 4,4′-(1,2-ethanediyl)bis(2,6-piperazinedione) using i.p.-i.p. models of P388 leukemia and B16 melanoma. As a result, we found 4,4′-(1,2-ethanediyl)bis(1-isobutoxycarbonyloxymethyl-2,6-piperazinedione) (MST-16) to possess considerable therapeutic activity. MST-16 showed not only marked life-prolonging effects in both P388 leukemia- and B16 melanoma-bearing mice but also a greater therapeutic ratio than did its parent compounds, ICRF-154 and ICRF-159. Further studies revealed that MST-16 has considerable therapeutic activity against a number of other tumors such as ascitic forms of L1210 leukemia, colon 26 adenocarcinoma, and MH-134 hepatoma and solid forms of B16 melanoma, Lewis lung carcinoma, colon 38 adenocarcinoma, and M5076 fibrosarcoma. These results suggest that MST-16 is very promising as an antitumor agent.

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Authors and Affiliations

  1. Research Laboratory, Zenyaku Kogyo Co., Ltd., 33-7 Ohizumi-machi 2-chome, Nerima-ku, 178, Tokyo, Japan

    Toshiharu Narita, Shin-ichi Yaguchi, Toshihiko Komatsu & Muneaki Takase

  2. Anjo Kosei Hospital, Anjo-shi, 446, Aichi, Japan

    Akira Hoshino

  3. Cancer Chemotherapy Center, Japanese Foundation for Cancer Research, Kami-Ikebukuro, Toshima-ku, 170, Tokyo, Japan

    Makoto Inaba & Shigeru Tsukagoshi

Authors
  1. Toshiharu Narita
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  2. Shin-ichi Yaguchi
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  3. Toshihiko Komatsu
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  4. Muneaki Takase
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  5. Akira Hoshino
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  6. Makoto Inaba
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  7. Shigeru Tsukagoshi
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Narita, T., Yaguchi, Si., Komatsu, T. et al. Antitumor activity of MST-16, a novel derivative of bis(2,6-dioxopiperazine), in murine tumor models. Cancer Chemother Pharmacol 26, 193–197 (1990). https://doi.org/10.1007/BF02897198

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  • DOI: https://doi.org/10.1007/BF02897198

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