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Elsevier, Bioorganic and Medicinal Chemistry Letters, 7(19), p. 2033-2037

DOI: 10.1016/j.bmcl.2009.02.028

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Antitumour and antimalarial activity of artemisinin–acridine hybrids

Journal article published in 2009 by Louise L. J. La Pensee, Michael Dr Jones, Amy E. Dr Mercer, Paul A. Dr Stocks, Paul M. O. Neill, Louise J. I. La Pensee, Rick Dr Cosstick, B. Kevin Prof Park, B. Kevin Park, Louise L. J. Dr La Pensee, Miriam E. Kennedy, Ivo Prof Piantanida ORCID, Stephen A. Prof Ward, Jill Davies, Patrick G. Dr Bray and other authors.
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This paper is available in a repository.

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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. (C) 2009 Elsevier Ltd. All rights reserved.