A newly developed hexamethylmelamine derivative, SAE9 with both antitumor and aromatase-inhibitory activity

H. Tanino, T. Kubota, Y. Yamada, J. I. Koh, T. Takeuchi, S. Kase, T. Furukawa, M. Takahashi, S. Fukuda, N. Ogose, T. Komatsu, M. Kato, M. Kitajima, T. Sakurai, Y. Naito, R. M. Hoffman

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Abstract

Hexamethylmelamine (HMM) has previously been shown to be active against ovarian, breast and small cell lung cancer. However HMM dose not have aromatase-inhibitory activity. A newly developed HMM derivative, 2-N, N-dimethylamino-4, 6-bis (1-H-imidazol-1-yl)-1,3,5- triazine (SAE9), was found to have direct antitumor activity as well as aromatase-inhibitory activity. The direct antitumor activity on breast carcinoma cell lines (MCF-7, R-27 and MDA-MB-231) was assessed using the 3-(4,5-dimethylthiazol-2yl)-2, 5-diphenyl tetrazolium bromide (MTT) on cells growing in monolayer culture. The 50% inhibitory concentrations (IC50) of SAE9 were found to be approximately 10-4 M for each cell line, roughly equivalent to those of HMM. When the aromatase-inhibitory effect was assessed using a human placental aromatase-inhibitory assay, the IC50 of SAE9 was 5.5 x 10-7 M, which was superior to that of aminoglutethimide (AG) (3.8 x 10-5 M). In a rat uterine growth model treated with androstenedione as the in vivo aromatase inhibition assay, SAE9 had an effect equivalent to that of AG. Since SAE9 has both antitumor and aromatase-inhibitory activity on breast carcinoma cell lines with estrogen dependency, this and similar non-steroidal aromatase inhibitors are thought to be promising for further study.

Original languageEnglish
Pages (from-to)623-626
Number of pages4
JournalAnticancer research
Volume13
Issue number3
Publication statusPublished - 1993 Jan 1

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Keywords

  • Aromatase-inhibitory activity
  • Hexamethylmelamine derivative
  • SAE9 antitumor activity

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

Cite this

Tanino, H., Kubota, T., Yamada, Y., Koh, J. I., Takeuchi, T., Kase, S., Furukawa, T., Takahashi, M., Fukuda, S., Ogose, N., Komatsu, T., Kato, M., Kitajima, M., Sakurai, T., Naito, Y., & Hoffman, R. M. (1993). A newly developed hexamethylmelamine derivative, SAE9 with both antitumor and aromatase-inhibitory activity. Anticancer research, 13(3), 623-626.