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Antitumour and antimalarial activity of artemisinin-acridine hybrids.

Authors :
Jones M
Mercer AE
Stocks PA
La Pensée LJ
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
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Apr 01; Vol. 19 (7), pp. 2033-7. Date of Electronic Publication: 2009 Feb 11.
Publication Year :
2009

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.

Details

Language :
English
ISSN :
1464-3405
Volume :
19
Issue :
7
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
19249201
Full Text :
https://doi.org/10.1016/j.bmcl.2009.02.028