Design, synthesis and evaluation of telomerase inhibitory, hTERT repressing, and anti-proliferation activities of symmetrical 1,8-disubstituted amidoanthraquinones

Chia Chung Lee, Kuo Feng Huang, Deh Ming Chang, Jung Jung Hsu, Fong Chun Huang, Kai Ning Shih, Chun Liang Chen, Tsung Chih Chen, Ruei Huei Chen, Jing Jer Lin, Hsu Shan Huang

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16 Citations (Scopus)

Abstract

A series of symmetrical disubstituded 1,8-diamidoanthraquinones were synthesized and evaluated for anti-proliferation, telomerase inhibitory by TRAP assay, and hTERT expression by SEAP assay. All of the compounds tested, except for compounds 3a and 3s were selected by the NCI screening system. In addition, compounds 4e and 4k exhibited inhibitory effects on telomerase activity. Taken together, our findings indicated that the analysis of cytotoxicity and telomerase inhibition might provide information applicable for further developing potential telomerase targeting strategy.

Original languageEnglish
Pages (from-to)102-112
Number of pages11
JournalEuropean Journal of Medicinal Chemistry
Volume50
DOIs
Publication statusPublished - Apr 2012
Externally publishedYes

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Keywords

  • Amidoanthraquinones
  • hTERT expression
  • NCI 60-cell panel assay
  • SEAP assay
  • Telomerase
  • TRAP assay

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

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