Antitumour and antimalarial activity of artemisinin-acridine hybrids

Bioorg Med Chem Lett. 2009 Apr 1;19(7):2033-7. doi: 10.1016/j.bmcl.2009.02.028. Epub 2009 Feb 11.

Abstract

Artemisinin-acridine hybrids were prepared and evaluated for their in vitro activity against tumour cell lines and a chloroquine sensitive strain of Plasmodium falciparum. They showed a 2-4-fold increase in activity against HL60, MDA-MB-231 and MCF-7 cells in comparison with dihydroartemisinin (DHA) and moderate antimalarial activity. Strong evidence that the compounds induce apoptosis in HL60 cells was obtained by flow cytometry, which indicated accumulation of cells in the G1 phase of the cell cycle.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acridines / chemical synthesis
  • Acridines / chemistry
  • Acridines / pharmacology*
  • Animals
  • Antimalarials / chemical synthesis
  • Antimalarials / chemistry*
  • Antimalarials / pharmacology*
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Apoptosis
  • Artemisinins / chemical synthesis
  • Artemisinins / chemistry
  • Artemisinins / pharmacology*
  • Cell Cycle
  • Cell Line, Tumor
  • Erythrocytes / drug effects
  • Flow Cytometry
  • G1 Phase
  • HL-60 Cells
  • Humans
  • Plasmodium falciparum / drug effects

Substances

  • Acridines
  • Antimalarials
  • Antineoplastic Agents
  • Artemisinins