RESUMEN

The first example of conjugation of open-resorcinarenes with chlorambucil, ibuprofen, naproxen and indomethacin are presented. The cytotoxic properties of the obtained conjugates were tested against the cancer cell lines U-251, PC-3, K-562, HCT-15, MCF-7 and SKLU-1. It was found that the conjugate with chlorambucil, naproxen or indomethacin (having 8 moieties) was toxic towards cancer cell lines U-251 and K-562, with no activity against non-cancerous COS-7 cells. The conjugates with naproxen and indomethacin showed high selectivity towards U-251 tumor cells.

Asunto(s)

Antineoplásicos/farmacología , Calixarenos/farmacología , Fenilalanina/análogos & derivados , Animales , Antineoplásicos/síntesis química , Antineoplásicos/química , Células COS , Calixarenos/síntesis química , Calixarenos/química , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Chlorocebus aethiops , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Estructura Molecular , Fenilalanina/síntesis química , Fenilalanina/química , Fenilalanina/farmacología , Relación Estructura-Actividad