ChloroquineV1, Main, Exploration, bibRecord, 002471

Antimalarial, Antitrypanosomal, and Antileishmanial Activities and Cytotoxicity of Bis(9-amino-6-chloro-2-methoxyacridines): Influence of the Linker#

Identifieur interne : 002471 ( Main/Exploration ); précédent : 002470; suivant : 002472

Antimalarial, Antitrypanosomal, and Antileishmanial Activities and Cytotoxicity of Bis(9-amino-6-chloro-2-methoxyacridines): Influence of the Linker#

Auteurs : Sophie Girault [Belgique] ; Philippe Grellier [Belgique] ; Amaya Berecibar [Belgique] ; Louis Maes [Belgique] ; Elisabeth Mouray [Belgique] ; Pascal Lemière [Belgique] ; Marie-Ange Debreu [Belgique] ; Elisabeth Davioud-Charvet [Belgique] ; Christian Sergheraert [Belgique, France]

Source :

Journal of Medicinal Chemistry [ 0022-2623 ] ; 2000.

RBID : ISTEX:D2AAC6B3D985D89F2FCF2ED09FF72A07FFFD56E0

Abstract

Forty bis(9-amino-6-chloro-2-methoxyacridines), in which acridine moieties are joined by alkanediamines, polyamines, or polyamines substituted by a side chain, were synthesized and tested for their in vitro activity upon the erythrocytic stage of Plasmodium falciparum, trypomastigote stage of Trypanosoma brucei, and amastigote stage of Trypanosoma cruzi and Leishmania infantum as well as for their cytotoxic effects upon MRC-5 cells. Results clearly showed the importance of the nature of the linker and of its side chain for antiparasitic activity, cytotoxicity, and cellular localization. Among several compounds devoid of cytotoxic effects at 25 μM upon MRC-5 cells, one displayed IC50 values ranging from 8 to 18 nM against different P. falciparum strains while three others totally inhibited T. brucei at 1.56 μM.

Url:

https://api.istex.fr/ark:/67375/TPS-GDW43MKP-L/fulltext.pdf

DOI: 10.1021/jm990946n

Affiliations:

Belgique, France

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Le document en format XML

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<front><div type="abstract">Forty bis(9-amino-6-chloro-2-methoxyacridines), in which acridine moieties are joined by alkanediamines, polyamines, or polyamines substituted by a side chain, were synthesized and tested for their in vitro activity upon the erythrocytic stage of Plasmodium falciparum, trypomastigote stage of Trypanosoma brucei, and amastigote stage of Trypanosoma cruzi and Leishmania infantum as well as for their cytotoxic effects upon MRC-5 cells. Results clearly showed the importance of the nature of the linker and of its side chain for antiparasitic activity, cytotoxicity, and cellular localization. Among several compounds devoid of cytotoxic effects at 25 μM upon MRC-5 cells, one displayed IC50 values ranging from 8 to 18 nM against different P. falciparum strains while three others totally inhibited T. brucei at 1.56 μM.</div>
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Antimalarial, Antitrypanosomal, and Antileishmanial Activities and Cytotoxicity of Bis(9-amino-6-chloro-2-methoxyacridines): Influence of the Linker#

Antimalarial, Antitrypanosomal, and Antileishmanial Activities and Cytotoxicity of Bis(9-amino-6-chloro-2-methoxyacridines): Influence of the Linker#

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Abstract

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