Inhibition of Tumor Cell Growth by A Specific 6-Phosphofructo-2-kinase Inhibitor, N-Bromoacetylethanolamine Phosphate, and Its Analogues.

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  • HIRATA Takafumi
    Department of Clinical Pharmaceutics, Graduate School of Pharmaceutical Sciences, Nagasaki University
  • WATANABE Mitsuaki
    Center for Instrumental Analysis, Nagasaki University
  • MIURA Shinji
    Biology Laboratory, Biochemicals Division, Yamasa Corporation
  • IJICHI Katsushi
    Biology Laboratory, Biochemicals Division, Yamasa Corporation
  • FUKASAWA Masashi
    Department of Microbiology, National Defense Medical College
  • SAKAKIBARA Ryuzo
    Department of Home Economics, Nutrition and Food Science Course, Kyushu Women’s University

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  • Inhibition of Tumor Cell Growth by A Specific 6-Phosphofructo-2-kinase Inhibitor,<i>N</i>-Bromoacetylethanolamine Phosphate, and Its Analogues

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Abstract

  The high rate of glycolysis despite the presence of oxygen and mitochondria in tumor cells implies an important role for this process in cell division. The rate of glycolysis is assumed to be dependent on the cellular concentration of fructose 2,6-bisphosphate, the concentration of which in turn depends on a bifunctional enzyme and the ratio of this enzyme’s 6-phosphofructo-2-kinase versus its fructose 2,6-bisphosphatase activities. To prove the hypothesis that inhibition of glycolysis in tumor cells by 6-phosphofructo-2-kinase inhibitors would cause inhibition of tumor cell proliferation, ten N-bromoacetylethanolamine phosphate analogues were designed, synthesized, and tested. They were screened for their activities against various human tumor cell lines to study the effects of inhibition of glycolysis on cell proliferation. The relationship between the structure of these compounds and their inhibitory activity on cell proliferation was also discussed. It was found that the activity of N-(2-methoxyethyl)-bromoacetamide, N-(2-ethoxyethyl)-bromoacetamide, and N-(3-methoxypropyl)-bromoacetamide was comparable to that of the positive control AraC. These three inhibitors showed in vivo anticancer effects in P388 transplant BDF1 mice.<br>

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