Development of 1-Amino-4-(phenylamino)anthraquinone-2-sulfonate Sodium Derivatives as a New Class of Inhibitors of RANKL-Induced Osteoclastogenesis

Chia Chung Lee, Chun Liang Chen, Fei Lan Liu, Chung Yu Chiou, Tsung Chih Chen, Cheng Chi Wu, Wei Hsin Sun, Deh Ming Chang, Hsu Shan Huang

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2 Citations (Scopus)


A series of 1-amino-4-(phenylamino)anthraquinone-2-sulfonate sodium derivatives was synthesized and evaluated for osteoclast inhibition using a TRAP-staining assay. Among them, two compounds, LCCY-13 and LCCY-15, dose-dependently suppressed receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclast formation. Moreover, the cytotoxicity assay on RAW264.7 cells suggested that the inhibition of osteoclastic bone resorption by these compounds was not a result of their cytotoxicity. Further, the inhibitory activities of compounds LCCY-13 and LCCY-15 were further confirmed by including specific inhibition of NFATc1 expression levels in nuclei using an immunofluorescent analysis. In addition, LCCY-13 and LCCY-15 also significantly attenuated the bone resorption activity of osteoclasts according to a pit formation assay. Thus, a new class of 1-amino-4-(phenylamino)anthraquinone-2-sulfonate sodium compounds might be considered as an essential lead structure for the further development of anti-resorptive agents.

Original languageEnglish
Pages (from-to)342-355
Number of pages14
JournalArchiv der Pharmazie
Issue number5
Publication statusPublished - May 1 2016



  • Anthraquinone derivatives
  • Osteoclastogenesis
  • TRAP-staining assay

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmaceutical Science

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