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Antitumour and antimalarial activity of artemisinin-acridine hybrids.
- 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.
- Subjects :
- Acridines chemical synthesis
Acridines chemistry
Animals
Antimalarials chemical synthesis
Antineoplastic Agents chemical synthesis
Apoptosis
Artemisinins chemical synthesis
Artemisinins chemistry
Cell Cycle
Cell Line, Tumor
Erythrocytes drug effects
Flow Cytometry
G1 Phase
HL-60 Cells
Humans
Plasmodium falciparum drug effects
Acridines pharmacology
Antimalarials chemistry
Antimalarials pharmacology
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Artemisinins pharmacology
Subjects
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