Chemical modification of dipeptide mimetic azatyrosine led to a series of piperazinediones. Thirteen piperazinediones were synthesized and tested for their anticancer activity. This series of piperazinedione compounds exhibited potent anticancer activities against human disease-oriented cancer cell lines in NCI60 cancer screening (National Cancer Institute, USA). Among them, four leads (compound 10, 18, 21, and 22) exhibited in vitro tumor growth suppression, reducing tumor cell growth to 45.7%-56.3%, and exhibited broad-spectrum activities. Compound 18, with 50% cancer cell growth inhibition (GI50)

Original languageEnglish
Pages (from-to)4013-4020
Number of pages8
JournalAnticancer Research
Issue number8
Publication statusPublished - Aug 1 2014


  • Azatyrosinamide
  • COMPARE algorithm
  • DTP
  • In vivo antitumor activity
  • Mechanism of action prediction
  • NCI-60 anticancer screening
  • Piperazinediones
  • Tubulin polymerization inhibitor

ASJC Scopus subject areas

  • Cancer Research
  • Oncology


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