Synthesis, telomerase evaluation and anti-proliferative studies on various series of diaminoanthraquinone-lkinked aminoacyl residue derivatives

Fong Chun Huang, Kuo Feng Huang, Ruey Hui Chen, Jia Er Wu, Tsung Chih Chen, Chun Liang Chen, Chia Chung Lee, Jin Yang Chen, Jing Jer Lin, Hsu Shan Huang

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

Four series of compounds containing an anthraquinone-linked moiety and symmetrical or asymmetrical aminoacyl residues in side chains at positions 1,4-, 1,5-, 2,6-, and 2,7- were synthesized and evaluated for their inhibitory effects toward telomerase and hTERT expression. Of these, only compound B11 showed selective inhibition of telomerase activity. Although it is not as competent as several of the anthraquinones we identified previously, nevertheless, the result is consistent with that the general structure moiety at the 1,5-position of diaminoanthraquinone-linked compound is important for the telomerase inhibitory activity. Interestingly, compounds A6, A8, C8, and D8 exhibited selective repressing activities toward hTERT expression and showed less effect toward proliferation of the treated cancer cells. Although it is not apparent which structure moiety is responsible for the telomerase repression effects of these compounds, they could be further developed as potential anti-tumor agents. This study shows how and to what extent the position of side chain substituents affects telomerase activity. Four series of compounds containing an anthraquinone-linked moiety and symmetrical or asymmetrical aminoacyl residues were synthesized and evaluated for their inhibitory effects towards telomerase and hTERT expression.

Original languageEnglish
Pages (from-to)101-111
Number of pages11
JournalArchiv der Pharmazie
Volume345
Issue number2
DOIs
Publication statusPublished - Feb 2012
Externally publishedYes

Keywords

  • Anthraquinone-linkage
  • Dose-dependent pattern
  • SEAP expression
  • Telomerase
  • TRAP assay

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmaceutical Science

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