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.

Michael Jones ¹, Amy E Mercer, Paul A Stocks, Louise J I La Pensée, Rick Cosstick, B Kevin Park, Miriam E Kennedy, Ivo Piantanida, Stephen A Ward, Jill Davies, Patrick G Bray, Sarah L Rawe, Jonathan Baird, Tafadzwa Charidza, Omar Janneh, Paul M O'Neill

Affiliations

Affiliation

1 Department of Chemistry, University of Liverpool, Crown Street, Liverpool L69 7ZD, UK.

PMID: 19249201 DOI: 10.1016/j.bmcl.2009.02.028

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.

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