A novel HIF-1 inhibitor - Manassantin A derivative LXY6099 inhibits tumor growth

Fang Fang Lai, Xiao Yu Liu, Fei Niu, Li Wei Lang, Ping Xie, Xiao Guang Chen

Research output: Contribution to journalArticlepeer-review

1 Scopus citations


Hypoxia-inducible factor-1 (HIF-1) is a key transcription factor on hypoxia responses in mammalian tissues. HIF-1 plays as a positive factor in solid tumor and leads to hypoxia-driven responses that enhance its downstream gene expression for tumor growth and survival. LXY6099 was obtained by the structural modification and optimization of manassantin A (MA) as a high potent HIF-1 inhibitor. Antitumor activity of LXY6099 was observed in this study. LXY6099 with an IC50 value of 2.46×10-10 mol·L -1 showed more sensitive inhibition activity to HIF-1 than that of MA detected by reporter gene assay (>100 folds). It showed strong inhibition on the growth of human solid tumor cell lines. Furthermore, LXY6099 exhibited significant antitumor activity against established human tumor xenografts in nu/nu mice with treatment of MX-1 breast cancer. Thus, LXY6099 as a novel HIF-1 inhibitor could be further developed into anti-cancer agents.

Original languageEnglish (US)
Pages (from-to)622-626
Number of pages5
JournalYaoxue Xuebao
Issue number5
StatePublished - May 12 2014
Externally publishedYes


  • Antitumor
  • Hypoxia-inducible factor-1
  • Inhibitor
  • Manassantin A derivative

ASJC Scopus subject areas

  • General Pharmacology, Toxicology and Pharmaceutics
  • Molecular Medicine


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