Azatyrosinamides: Novel RAS-related anticancer agents

Chun Li Wang, On Lee, Chiu Fen Huang, Eric I Chian Li, Che Ming Teng, Shiow Lin Pan, Jang Feng Lian, Feng Shou Chang, Jing Ping Liou, Hui Po Wang

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2 Citations (Scopus)


Background: We previously reported on the design and synthesis of novel azatyrosinamide derivatives selective for ras-transformed NIH3T3 cells and with improved toxicity over azatyrosine. This study was aimed at investigating the mechanism of action and the antitumour activity of these compounds in ras-transformed cells. Materials and Methods: Nine azatyrosinamides were previously screened for anticancer activity in both wild-type and ras-transformed NIH3T3 cells; the most active compounds were further tested in vitro and in vivo. Results: HPW98-1 and HPW98-2 induced formation of apoptotic bodies in ras-transformed NIH3T3 cells in vitro and inhibited anchorage-independent growth. Excess tyrosine reduced the cytotoxic effect of azatyrosine, but not of HPW98-1 and HPW98-2. HPW98-1 reduced vascular endothelial growth factor-mediated angiogenesis in a Matrigel plug assay and attenuated growth of a ras-transformed NIH3T3 xenograft and a human SW620 xenograft. Conclusion: Our results support the continued study of HPW98-1 for its potential use in the treatment of RAS-related cancers.

Original languageEnglish
Pages (from-to)425-432
Number of pages8
JournalAnticancer Research
Issue number2
Publication statusPublished - Feb 2013


  • Angiogenesis
  • Antitumour agent
  • Azatyrosinamides
  • NIH3T3
  • Ras
  • SW620 human colon xenograft

ASJC Scopus subject areas

  • Cancer Research
  • Oncology

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  • Cite this

    Wang, C. L., Lee, O., Huang, C. F., Li, E. I. C., Teng, C. M., Pan, S. L., Lian, J. F., Chang, F. S., Liou, J. P., & Wang, H. P. (2013). Azatyrosinamides: Novel RAS-related anticancer agents. Anticancer Research, 33(2), 425-432.