Structure-based design, synthesis and biological evaluation of novel anthra[1,2-d]imidazole-6,11-dione homologues as potential antitumor agents

Tsung Chih Chen, Dah Shyong Yu, Kuo Feng Huang, Yung Chien Fu, Chia Chung Lee, Chun Liang Chen, Fong Chun Huang, Hsi Hsien Hsieh, Jing Jer Lin, Hsu Shan Huang

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18 Citations (Scopus)

Abstract

By using fragment-based design strategies, a series of 2-thio-substituted anthra[1,2-d]imidazole-6,11-diones were synthesized and evaluated for hTERT repressing activities, cell proliferations, and NCI 60-cell panel assay. Compounds 2, 3, 4, 11, 15 and 35 were selected by the NCI and 3, 4, 11 and 15 represent the GI50, TGI and LC50, respectively. Among them, all were moderate selectivity toward leukemia cancer except for 4 exhibited distinctive selectivity of CNS and renal cancer with 7.403 and 6.475. The overall of test compounds exhibited different cytostatic and cytotoxic activities for further developing potential application as anticancer drugs.

Original languageEnglish
Pages (from-to)278-293
Number of pages16
JournalEuropean Journal of Medicinal Chemistry
Volume69
DOIs
Publication statusPublished - 2013
Externally publishedYes

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Keywords

  • Anthra 12-dimidazole-611-dione
  • Cytostatic and cytotoxic activities
  • NCI 60-cell panel assay
  • Selectivity ratio

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

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