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

doi:10.1016/j.ejmech.2014.07.105

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 journal › Article › peer-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 language	English
Pages (from-to)	289-92
Number of pages	4
Journal	European Journal of Medicinal Chemistry
Volume	85
DOIs	https://doi.org/10.1016/j.ejmech.2014.07.105
Publication status	Published - 6 Oct 2014

Keywords

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

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title = "In vitro antiplasmodial and cytotoxic activities of asymmetrical pyridinium derivatives",

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.",

keywords = "Animals, Antimalarials, Cell Line, Humans, Inhibitory Concentration 50, Plasmodium falciparum, Pyridinium Compounds, Rats",

author = "Bel{\'e}n Rubio-Ruiz and Castillo-Acosta, {V{\'i}ctor M} and Guiomar P{\'e}rez-Moreno and Antonio Espinosa and Dolores Gonz{\'a}lez-Pacanowska and Ruiz-P{\'e}rez, {Luis M} and Antonio Entrena and Ana Conejo-Garc{\'i}a",

year = "2014",

month = oct,

day = "6",

doi = "10.1016/j.ejmech.2014.07.105",

language = "English",

volume = "85",

pages = "289--92",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson SAS",

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In vitro antiplasmodial and cytotoxic activities of asymmetrical pyridinium derivatives. / Rubio-Ruiz, Belén; Castillo-Acosta, Víctor M; Pérez-Moreno, Guiomar; Espinosa, Antonio; González-Pacanowska, Dolores; Ruiz-Pérez, Luis M; Entrena, Antonio; Conejo-García, Ana.

In: European Journal of Medicinal Chemistry, Vol. 85, 06.10.2014, p. 289-92.

Research output: Contribution to journal › Article › peer-review

TY - JOUR

T1 - In vitro antiplasmodial and cytotoxic activities of asymmetrical pyridinium derivatives

AU - Rubio-Ruiz, Belén

AU - Castillo-Acosta, Víctor M

AU - Pérez-Moreno, Guiomar

AU - Espinosa, Antonio

AU - González-Pacanowska, Dolores

AU - Ruiz-Pérez, Luis M

AU - Entrena, Antonio

AU - Conejo-García, Ana

PY - 2014/10/6

Y1 - 2014/10/6

N2 - 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.

AB - 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.

KW - Animals

KW - Antimalarials

KW - Cell Line

KW - Humans

KW - Inhibitory Concentration 50

KW - Plasmodium falciparum

KW - Pyridinium Compounds

KW - Rats

U2 - 10.1016/j.ejmech.2014.07.105

DO - 10.1016/j.ejmech.2014.07.105

M3 - Article

C2 - 25089811

VL - 85

SP - 289

EP - 292

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

SN - 0223-5234

ER -