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Antitumour and antimalarial activity of artemisinin-acridine hybrids

Jones, M., Mercer, A. E., Stocks, Paul A., La Pensee, L. J. I., Cosstick, R., Park, B. K., Kennedy, M. E., Piantanida, I., Ward, Stephen ORCID: https://orcid.org/0000-0003-2331-3192, Davies, Jill, Bray, Patrick, Rawe, S. L., Baird, J., Charidza, T., Janneh, O. and O'Neill, P. M. (2009) 'Antitumour and antimalarial activity of artemisinin-acridine hybrids'. Bioorganic & Medicinal Chemistry Letters, Vol 19, Issue 7, pp. 2033-2037.

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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.

Item Type: Article
Uncontrolled Keywords: artemisinin acridine antimalarial anticancer apoptosis DNA confocal microscopy tumor-cells DNA cytotoxicity dihydroartemisinin intercalation endoperoxides derivatives artesunate complexes chemistry
Subjects: QZ Pathology > Neoplasms. Cysts > QZ 200 Neoplasms. Cysts (General)
QV Pharmacology > Anti-Inflammatory Agents. Anti-Infective Agents. Antineoplastic Agents > QV 256 Antimalarials
QV Pharmacology > Anti-Inflammatory Agents. Anti-Infective Agents. Antineoplastic Agents > QV 254 Antiprotozoal agents (General)
Faculty: Department: Groups (2002 - 2012) > Molecular & Biochemical Parasitology Group
Digital Object Identifer (DOI): https://doi.org/10.1016/j.bmcl.2009.02.028
Depositing User: Mary Creegan
Date Deposited: 24 Jun 2010 14:34
Last Modified: 06 Feb 2018 12:59
URI: https://archive.lstmed.ac.uk/id/eprint/293

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