Structure-based hybridization, synthesis and biological evaluation of novel tetracyclic heterocyclic azathioxanthone analogues as potential antitumor agents

Tsung Chih Chen, Chia Lun Wu, Chia Chung Lee, Chun Liang Chen, Dah Shyong Yu, Hsu Shan Huang

Research output: Contribution to journalArticle

17 Citations (Scopus)


A series of tetracyclic heterocyclic azathioxanthones were synthesized and evaluated for cell proliferations, topoisomerase inhibitions, and NCI-60 cell panel assay, respectively. Compounds 5, 7, 8, 16, and 19 were selected for topoisomerase assay after MTT assay. 7 not only showed cytotoxic effect (IC50 Combining double low line 2.84 ± 0.64 μM) in PC-3 cells but also revealed topoisomerases inhibition with IC50 (10-25 μM) and increased apoptotic cleavage of PARP and caspase 3 activity. The overall of novel azathioxanthones with different cytostatic and cytotoxic activities should be further developed as new potential candidates for anticancer drugs.

Original languageEnglish
Pages (from-to)615-627
Number of pages13
JournalEuropean Journal of Medicinal Chemistry
Publication statusPublished - Oct 20 2015



  • Azathioxanthones
  • Cytostatic and cytotoxic activities
  • MTT assay
  • NCI-60 human tumor cell lines
  • Topoisomerase assays

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

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