ChloroquineV1, Main, Exploration, bibRecord, 002285

Antiplasmodial Activity and Cytotoxicity of Bis-, Tris-, and Tetraquinolines with Linear or Cyclic Amino Linkers

Identifieur interne : 002285 ( Main/Exploration ); précédent : 002284; suivant : 002286

Antiplasmodial Activity and Cytotoxicity of Bis-, Tris-, and Tetraquinolines with Linear or Cyclic Amino Linkers

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

Source :

Journal of Medicinal Chemistry [ 0022-2623 ] ; 2001.

RBID : ISTEX:0A2A8BD78C7DDE4E4D3F300108747C1BA26F1032

Abstract

Bisquinoline heteroalkanediamines were structurally modified in order to study the effects of enhanced bulkiness and rigidity on both their activity on strains of Plasmodium falciparum expressing different degrees of chloroquine (CQ) resistance and their cytotoxicity toward mammalian cells. While cyclization yielded molecules of greater rigidity that were not more active than their linear counterparts, they were characterized by an absence of cytotoxicity. Alternatively, dimerization of these compounds led to tetraquinolines that are very potent for CQ-resistant strains and noncytotoxic.

Url:

https://api.istex.fr/ark:/67375/TPS-V78BD7W8-B/fulltext.pdf

DOI: 10.1021/jm001096a

Affiliations:

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Le document en format XML

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Antiplasmodial Activity and Cytotoxicity of Bis-, Tris-, and Tetraquinolines with Linear or Cyclic Amino Linkers

Antiplasmodial Activity and Cytotoxicity of Bis-, Tris-, and Tetraquinolines with Linear or Cyclic Amino Linkers

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