Novel synthetic acridine derivatives as potent DNA-binding and apoptosis-inducing antitumor agents

Bioorg Med Chem. 2013 Jul 15;21(14):4170-7. doi: 10.1016/j.bmc.2013.05.008. Epub 2013 May 16.


Acridine derivatives have been explored as DNA-binding anticancer agents. Some derivatives show undesired pharmacokinetic properties and new derivatives need to be explored. In this work, a series of novel acridine analogues were synthesized by modifying previously unexplored linkers between the acridine and benzene groups and their antiproliferative activity and the DNA-binding ability were evaluated. Among these derivatives, compound 5c demonstrated DNA-binding capability and topoisomerase I inhibitory activity. In K562 cell lines, 5c induced apoptosis through mitochondria-dependent intrinsic pathways. These data suggested that compound 5c and other acridine derivatives with modified linkers between the acridine and benzene groups might be potent DNA-binding agents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acridines / chemistry*
  • Acridines / metabolism
  • Acridines / pharmacology*
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / metabolism
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects*
  • Circular Dichroism
  • DNA / chemistry
  • DNA / metabolism*
  • Humans
  • K562 Cells
  • Molecular Structure


  • Acridines
  • Antineoplastic Agents
  • DNA