Antitumour and antimalarial activity of artemisinin-acridine hybrids

Michael Jones; 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

doi:10.1016/j.bmcl.2009.02.028

Antitumour and antimalarial activity of artemisinin-acridine hybrids

Michael Jones, 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

Research output: Contribution to journal › Article › peer-review

62 Citations (Scopus)

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.

Original language	English
Pages (from-to)	2033-2037
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Issue number	7
DOIs	https://doi.org/10.1016/j.bmcl.2009.02.028
Publication status	Published - 1 Apr 2009

Keywords

Acridine
Anticancer
Antimalarial
Apoptosis
Artemisinin
Confocal microscopy
DNA

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10.1016/j.bmcl.2009.02.028

https://arrow.tudublin.ie/scschcpsart/17Licence: CC BY-NC-SA

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Jones, M., Mercer, A. E., Stocks, P. A., La Pensée, L. J. I., Cosstick, R., Park, B. K., Kennedy, M. E., Piantanida, I., Ward, S. A., Davies, J., Bray, P. G., Rawe, S. L., Baird, J., Charidza, T., Janneh, O., & O'Neill, P. M. (2009). Antitumour and antimalarial activity of artemisinin-acridine hybrids. Bioorganic and Medicinal Chemistry Letters, 19(7), 2033-2037. https://doi.org/10.1016/j.bmcl.2009.02.028

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title = "Antitumour and antimalarial activity of artemisinin-acridine hybrids",

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.",

keywords = "Acridine, Anticancer, Antimalarial, Apoptosis, Artemisinin, Confocal microscopy, DNA",

author = "Michael Jones and Mercer, {Amy E.} and Stocks, {Paul A.} and {La Pens{\'e}e}, {Louise J.I.} and Rick Cosstick and Park, {B. Kevin} and Kennedy, {Miriam E.} and Ivo Piantanida and Ward, {Stephen A.} and Jill Davies and Bray, {Patrick G.} and Rawe, {Sarah L.} and Jonathan Baird and Tafadzwa Charidza and Omar Janneh and O'Neill, {Paul M.}",

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doi = "10.1016/j.bmcl.2009.02.028",

language = "English",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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Jones, M, Mercer, AE, Stocks, PA, La Pensée, LJI, Cosstick, R, Park, BK, Kennedy, ME, Piantanida, I, Ward, SA, Davies, J, Bray, PG, Rawe, SL, Baird, J, Charidza, T, Janneh, O & O'Neill, PM 2009, 'Antitumour and antimalarial activity of artemisinin-acridine hybrids', Bioorganic and Medicinal Chemistry Letters, vol. 19, no. 7, pp. 2033-2037. https://doi.org/10.1016/j.bmcl.2009.02.028

TY - JOUR

T1 - Antitumour and antimalarial activity of artemisinin-acridine hybrids

AU - Jones, Michael

AU - Mercer, Amy E.

AU - Stocks, Paul A.

AU - La Pensée, Louise J.I.

AU - Cosstick, Rick

AU - Park, B. Kevin

AU - Kennedy, Miriam E.

AU - Piantanida, Ivo

AU - Ward, Stephen A.

AU - Davies, Jill

AU - Bray, Patrick G.

AU - Rawe, Sarah L.

AU - Baird, Jonathan

AU - Charidza, Tafadzwa

AU - Janneh, Omar

AU - O'Neill, Paul M.

PY - 2009/4/1

Y1 - 2009/4/1

N2 - 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.

AB - 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.

KW - Acridine

KW - Anticancer

KW - Antimalarial

KW - Apoptosis

KW - Artemisinin

KW - Confocal microscopy

KW - DNA

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U2 - 10.1016/j.bmcl.2009.02.028

DO - 10.1016/j.bmcl.2009.02.028

M3 - Article

C2 - 19249201

AN - SCOPUS:62149130062

SN - 0960-894X

VL - 19

SP - 2033

EP - 2037

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 7

ER -

Antitumour and antimalarial activity of artemisinin-acridine hybrids

Abstract

Keywords

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