Ring fusion strategy for synthesis and lead optimization of sulfur-substituted anthra[1,2-c[[1,2,5]thiadiazole-6,11-dione derivatives as promising scaffold of antitumor agents

Yu Ru Lee, Tsung Chih Chen, Chia Chung Lee, Chun Liang Chen, Ahmed Atef Ahmed Ali, Alexander Tikhomirov, Jih Hwa Guh, Dah Shyong Yu, Hsu Shan Huang

Research output: Contribution to journalArticle

14 Citations (Scopus)

Abstract

A series of sulfur-substituted anthra[1,2-c][1,2,5]thiadiazole-6,11-diones were synthesized and evaluated using the cell proliferations, apoptosis and NCI-60 cell panel assays. Also, the signaling pathways that account for their activities were investigated. Compounds 2, 3, 4a, 4d, 4f, 4i, 4k, 5b, 5c, 5d, 5f, 5g, 6b, 6c, 6d, 6e, 6g, 7a and 7g were selected by NCI. Among the tested compounds, 6g appeared to be the most active compound of this series that not only induced apoptosis in DU-145 cancer cells but also attenuated the ERK1/2 and p38 signaling pathways. All test compounds exhibited diverse cytostatic and cytotoxic activities that warrant further development as potential anticancer agents.

Original languageEnglish
Pages (from-to)661-676
Number of pages16
JournalEuropean Journal of Medicinal Chemistry
Volume102
DOIs
Publication statusPublished - Sep 18 2015

Keywords

  • Anthra[1 2-c][1 2 5]thiadiazole-6 11-dione
  • Apoptosis
  • NCI 60-cell panel assay
  • SRB assay
  • Thiadiazoles

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

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