In vitro antiplasmodial and cytotoxic activities of asymmetrical pyridinium derivatives

Belén Rubio-Ruiz, Víctor M Castillo-Acosta, Guiomar Pérez-Moreno, Antonio Espinosa, Dolores González-Pacanowska, Luis M Ruiz-Pérez, Antonio Entrena, Ana Conejo-García

Research output: Contribution to journalArticlepeer-review

Abstract

An in vitro investigation of the antiplasmodial and cytotoxic activities of a series of human choline kinase inhibitors against Plasmodium falciparum is reported. Structure-activity relationship analyses have allowed us to determine the essential parameters for the antimalarial effect of these asymmetrical pyridinium derivatives. One of the compounds meets the World Health Organization's criteria for hit identification against P. falciparum exhibiting an IC50 of 0.0016 μg/ml and a selectivity index of >3000.

Original languageEnglish
Pages (from-to)289-92
Number of pages4
JournalEuropean Journal of Medicinal Chemistry
Volume85
DOIs
Publication statusPublished - 6 Oct 2014

Keywords

  • Animals
  • Antimalarials
  • Cell Line
  • Humans
  • Inhibitory Concentration 50
  • Plasmodium falciparum
  • Pyridinium Compounds
  • Rats

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