Design, synthesis and antiproliferative evaluation of fluorenone analogs with DNA topoisomerase i inhibitory properties

Chia Chung Lee, Deh Ming Chang, Kuo Feng Huang, Chun Liang Chen, Tsung Chih Chen, Yang Lo, Jih Hwa Guh, Hsu Shan Huang

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

A series of 2,7-diamidofluorenones were designed, synthesized, and screened by SRB assay. Some synthesized compounds exhibited antitumor activities in submicromolar range. Ten compounds (3a, 3b, 3c, 3g, 3j, 3l, 4a, 4h, 4i, and 4j) were also selected by NCI screening system and 3c (GI50 = 1.66 μM) appeared to be the most active agent of this series. Furthermore, 3c attenuated topoisomerase I-mediated DNA relaxation at low micromolar concentrations. These results indicated that fluorenones have potential to be further developed into anticancer drugs.

Original languageEnglish
Pages (from-to)7125-7133
Number of pages9
JournalBioorganic and Medicinal Chemistry
Volume21
Issue number22
DOIs
Publication statusPublished - Nov 15 2013
Externally publishedYes

Keywords

  • Fluorenones
  • NCI 60-cell panel assay
  • Tilorone
  • Topoisomerase I

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

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