Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 1 de 1
Filtrar
Más filtros












Base de datos
Intervalo de año de publicación
1.
Bioorg Med Chem Lett ; 30(11): 127149, 2020 06 01.
Artículo en Inglés | MEDLINE | ID: mdl-32247731

RESUMEN

A broad range of chalcones and derivatives were easily and rapidly synthesized, following Claisen-Schmidt condensation of (hetero)aryl ketones and (hetero)aryl aldehydes using a ultrasound probe. A comparison was made with classical magnetic stirring experiments, and an optimization study was realized, showing lithium hydroxide to be the best basic catalyst of the studied condensations. By-products of the reactions (ß-hydroxy-ketone, diketones, and cyclohexanols) were also isolated. All compounds were evaluated in vitro for their ability to inhibit human farnesyltransferase, a protein implicated in cancer and rare diseases and on the NCI-60 cancer cell lines panel. Molecules showed inhibitory activity on the target protein and cytostatic effect on different cell lines with particular activity against MCF7, breast cancer cells.


Asunto(s)
Antineoplásicos/síntesis química , Chalconas/química , Inhibidores Enzimáticos/síntesis química , Farnesiltransferasa/antagonistas & inhibidores , Antineoplásicos/metabolismo , Antineoplásicos/farmacología , Sitios de Unión , Dominio Catalítico , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Chalconas/metabolismo , Chalconas/farmacología , Ensayos de Selección de Medicamentos Antitumorales , Inhibidores Enzimáticos/metabolismo , Inhibidores Enzimáticos/farmacología , Farnesiltransferasa/metabolismo , Humanos , Simulación del Acoplamiento Molecular , Sonicación , Relación Estructura-Actividad
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA
...