Literature DB >> 19249201

Antitumour and antimalarial activity of artemisinin-acridine hybrids.

Michael Jones1, 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.   

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.

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Year:  2009        PMID: 19249201     DOI: 10.1016/j.bmcl.2009.02.028

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

1.  Synthesis of a potent antimalarial agent through natural products conjugation.

Authors:  Michela Bruno; Beatrice Trucchi; Diego Monti; Sergio Romeo; Marcel Kaiser; Luisella Verotta
Journal:  ChemMedChem       Date:  2013-01-10       Impact factor: 3.466

2.  Next-Generation Antimalarial Drugs: Hybrid Molecules as a New Strategy in Drug Design.

Authors:  Francis W Muregi; Akira Ishih
Journal:  Drug Dev Res       Date:  2010-02       Impact factor: 4.360

Review 3.  Peroxides with Anthelmintic, Antiprotozoal, Fungicidal and Antiviral Bioactivity: Properties, Synthesis and Reactions.

Authors:  Vera A Vil'; Ivan A Yaremenko; Alexey I Ilovaisky; Alexander O Terent'ev
Journal:  Molecules       Date:  2017-11-02       Impact factor: 4.411

Review 4.  Acridine-Based Antimalarials-From the Very First Synthetic Antimalarial to Recent Developments.

Authors:  Mélanie Fonte; Natália Tassi; Paula Gomes; Cátia Teixeira
Journal:  Molecules       Date:  2021-01-24       Impact factor: 4.411

5.  Heme mediates cytotoxicity from artemisinin and serves as a general anti-proliferation target.

Authors:  Shiming Zhang; Glenn S Gerhard
Journal:  PLoS One       Date:  2009-10-28       Impact factor: 3.240

Review 6.  Artemisinin and Derivatives-Based Hybrid Compounds: Promising Therapeutics for the Treatment of Cancer and Malaria.

Authors:  Sijongesonke Peter; Siphesihle Jama; Sibusiso Alven; Blessing A Aderibigbe
Journal:  Molecules       Date:  2021-12-11       Impact factor: 4.411

  6 in total

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