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 引文 斯高帕斯(Scopus)

摘要

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.
原文英語
頁(從 - 到)425-432
頁數8
期刊Anticancer Research
33
發行號2
出版狀態已發佈 - 二月 2013

ASJC Scopus subject areas

  • 腫瘤科
  • 癌症研究

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