Evaluation of Antimalarial and Cytotoxic Activity of Styrylquinolines obtained from 8-Hydroxyquinaldine with Aromatic Aldehydes

Abstract

This study reports the synthesis of five (E)-Styrylquinolines (Q.1, Q.2, Q.3, Q.5, Q.6) and three O-alkylated derivatives (Q.1a, Q.6a, Q 6 b) and the evaluation of its antimalarial activity and cytotoxic in vitro -- For Styrylquinolines Perkin condensation reaction type from 8-hydroxyquinaldine with aromatic aldehydes was used -- Antimalarial activity was performed using the method Radioisotope with FCB-2 strains of Plasmodium falciparum (chloroquine-resistant) and for the cytotoxic activity the MTT method with HepG2 cells was employed -- Most compounds showed to be active antimalarial -- Those with higher activity were Q.3 (IC506.4μM) and Q.5 (IC5010.8 µM), although all of them were cytotoxic at concentrations above 1 µg / mL -- The structures of these compounds were confirmed using infrared spectroscopy techniques and MRI in one and two dimensions

El presente estudio reporta la síntesis de cinco (E)-estirilquinolinas (Q.1, Q.2, Q.3, Q.5, Q.6) y tres derivados O-alquilados (Q.1a, Q.6a, Q.6b) y la evaluación de su actividad antimalárica y citotóxica in vitro -- Para obtener las estirilquinolinas se empleó la reacción de condensación tipo Perkin a partir de 8-hidroxiquinaldina con aldehídos aromáticos -- La actividad antimalárica se realizó empleando el método Radioisotópico con cepas FCB-2 de Plasmodium falciparum (resistente a la cloroquina) y para la actividad citotóxica se empleó el método del MTT con células HepG2 -- La mayoría de los compuestos mostraron ser activos antimaláricos -- Los que presentan mayor actividad son el Q.3 (IC50 6.4µM), y el Q.5 (IC5010.8 µM) aunque todos mostraron ser citotóxicos a concentraciones superiores a 1µg/mL -- Las estructuras de estos compuestos se confirmaron empleando técnicas espectroscópicas de Infrarrojo y Resonancia Magnética Nuclear en una y dos dimensiones