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.
Richard K Amewu  1 ,  James Chadwick ,  Afthab Hussain ,  Somnath Panda ,  Rinki Rinki ,  Omar Janneh ,  Stephen A Ward ,  Candel Miguel ,  Hollie Burrell-Saward ,  Livia Vivas ,  Paul M O'Neill
Affiliations
  • 1. Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, UK. Electronic address: [email protected].
PMID: 24148834 DOI: 10.1016/j.bmc.2013.09.047
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.