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*

*Corresponding author for this work

Research output: Contribution to journalJournal Article peer-review

2 Scopus citations


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
StatePublished - 02 2013
Externally publishedYes


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


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