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Titre du document / Document title

Quinoxaline chemistry. Part 8. 2-[anilino]-3-[carboxy]-6(7)-substituted quinoxalines as non classical antifolate agents. Synthesis and evaluation of in vitro anticancer, anti-HIV and antifungal activity

Auteur(s) / Author(s)

LORIGA M. (1) ; MORO P. (1) ; SANNA P. (1) ; PAGLIETTI G. (1) ; ZANETTI S. (2) ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

(1) Istituto di Chimica Farmaceutica, Università di Sassari, Via Muroni 23/A, 07100 Sassari, ITALIE
(2) Istituto di Microbiologia e Virologia delta Facoltà di Medicina, Viale S. Pietro, 07100 Sassari, ITALIE

Résumé / Abstract

Thirty quinoxalines bearing a substituted anilino group on position 2, a carboethoxy or carboxy group on position 3 and a trifluoromethyl group on position 6 or 7 of the heterocycle were prepared in order to evaluate in vitro anticancer activity. Preliminary screening performed at NCI showed that most derivatives exhibited a moderate to strong growth inhibition activity on various tumor panel cell lines between 10-5 and 10-4 molar concentrations. Interesting selectivities were also recorded between 10-8 and 10-6 M for a few compounds. One single compound exhibited good activity against Candida Albicans

Revue / Journal Title

Il Farmaco    ISSN  0014-827X 

Source / Source

1997, vol. 52, no8-9, pp. 531-537 (9 ref.)

Langue / Language

Anglais

Editeur / Publisher

Elsevier, Lausanne, SUISSE  (1989-2005) (Revue)

Mots-clés anglais / English Keywords

Structure activity relation

;

Antineoplastic agent

;

In vitro

;

Established cell line

;

Tumor cell

;

Human

;

Antifungal agent

;

Candida albicans

;

Chemical synthesis

;

Quinoxaline derivatives

;

Nitrogen heterocycle

;

Bicyclic compound

;

Aromatic compound

;

Fluorine Organic compounds

;

Fungi Imperfecti

;

Fungi

;

Thallophyta

;

Mots-clés français / French Keywords

Relation structure activité

;

Anticancéreux

;

In vitro

;

Lignée cellulaire établie

;

Cellule tumorale

;

Homme

;

Antifongique

;

Candida albicans

;

Synthèse chimique

;

Quinoxaline dérivé

;

Hétérocycle azote

;

Composé bicyclique

;

Composé aromatique

;

Fluor Composé organique

;

Quinoxaline-2-carboxylique acide(3-arylamino) ester éthyle

;

Quinoxaline-2-carboxylique acide(3-[4-fluoroanilino]-7-trifluorométhyl)

;

Fungi Imperfecti

;

Fungi

;

Thallophyta

;

Mots-clés espagnols / Spanish Keywords

Relación estructura actividad

;

Anticanceroso

;

In vitro

;

Línea celular establecida

;

Célula tumoral

;

Hombre

;

Antifúngico

;

Candida albicans

;

Síntesis química

;

Quinoxalina derivado

;

Heterociclo nitrógeno

;

Compuesto bicíclico

;

Compuesto aromático

;

Fluor Compuesto orgánico

;

Fungi Imperfecti

;

Fungi

;

Thallophyta

;

Localisation / Location

INIST-CNRS, Cote INIST : 3341, 35400007819007.0040

Nº notice refdoc (ud4) : 2137306



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