Synthesis and evaluation of the antimalarial, anticancer, and caspase 3 activities of tetraoxane dimers

Bioorg Med Chem. 2013 Dec 1;21(23):7392-7. doi: 10.1016/j.bmc.2013.09.047. Epub 2013 Oct 1.

Abstract

The synthesis of a range of mono spiro and dispiro 1,2,4,5-tetraoxane dimers is described. Selected molecules were examined in in vitro assays to determine their antimalarial and anticancer potential. Our studies reveal that several molecules possess potent nanomolar antimalarial and single digit micromolar antiproliferative IC(50)s versus colon (HT29-AK and leukemia (HL60) cell lines.

Keywords: Apoptosis; Leukaemia; Malaria.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antimalarials / chemical synthesis
  • Antimalarials / chemistry*
  • Antimalarials / pharmacology*
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Caspase 3 / metabolism*
  • Cell Line, Tumor
  • Dimerization
  • Humans
  • Malaria, Falciparum / drug therapy
  • Neoplasms / drug therapy
  • Plasmodium falciparum / drug effects
  • Tetraoxanes / chemical synthesis
  • Tetraoxanes / chemistry*
  • Tetraoxanes / pharmacology*

Substances

  • Antimalarials
  • Antineoplastic Agents
  • Tetraoxanes
  • Caspase 3