Synthesis, antiproliferative activities and telomerase inhibition evaluation of novel asymmetrical 1,2-disubstituted amidoanthraquinone derivatives

Chia Chung Lee, Kuo Feng Huang, Pen Yuan Lin, Fong Chun Huang, Chun Liang Chen, Tsung Chih Chen, Jih Hwa Guh, Jing Jer Lin, Hsu Shan Huang

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21 Citations (Scopus)

Abstract

A series of diversely asymmetrical mono- or disubstituted 1,2-diamidoanthraquinone derivatives were synthesized and evaluated for drug-induced cytotoxicity by SRB assay, telomerase inhibitory activity by TRAP assay, and hTERT expression by SEAP assay. Interestingly, compounds 4, 11, 21, 32 and 36 exhibited selective potent antiproliferative activities by NCI with IC 50 values in the micromolar range. Of these, only compound 8 showed an IC 50 value of 0.95 μM against PC-3 cell lines (human prostate cancer) by SRB assay. All the synthesized compounds exhibited a poor or modest telomerase inhibitory activity by TRAP assay suggesting another mode of action for these compounds. Compound 11 showed broad inhibition against different types of cancer cell lines in the micromolar and submicromolar range.

Original languageEnglish
Pages (from-to)323-336
Number of pages14
JournalEuropean Journal of Medicinal Chemistry
Volume47
Issue number1
DOIs
Publication statusPublished - Jan 2012

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Keywords

  • Anthraquinone
  • NCI 60-cell panel assay
  • Sulforhodamine B (SRB) assay
  • Telomerase activity
  • TRAP assay

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

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