RESUMEN

A large series of alkyl C-glycosides was synthesized from D-glucal or D-galactal. These compounds were screened against the human promyelocytic leukemia cell line (HL60), showing significant activity and apoptosis. Up to 13 C-glucopyranosides, but no C-galacto- or C-mannopyranosides, exhibited inhibitory concentrations (IC(50) values) below 20 microM, five of them in the range 4-8 microM. Preliminary structure-activity relationships were established.

Asunto(s)

Antineoplásicos/farmacología , Glicósidos/química , Leucemia/tratamiento farmacológico , Leucemia/metabolismo , Leucemia/patología , Apoptosis , Línea Celular Tumoral , Proliferación Celular , Ensayos de Selección de Medicamentos Antitumorales , Células HL-60 , Humanos , Concentración 50 Inhibidora , Cetonas , Modelos Químicos , Relación Estructura-Actividad