RESUMEN

Analogs of the antitumor agents cryptophycins 1 and 8 with dialkyl substitution at C-6 (fragment C) were synthesized and evaluated for in vitro cytotoxicity against human leukemia cells (CCRF-CEM). The activity of these analogs decreased as the size of the substituents at C-6 increased. The C-6 spirocylopropyl compound (2g) was highly potent in vitro and showed excellent antitumor activity in animal models.

Asunto(s)

Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Péptidos Cíclicos/síntesis química , Péptidos Cíclicos/farmacología , Animales , Antineoplásicos/química , Depsipéptidos , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Ratones , Péptidos Cíclicos/química , Células Tumorales Cultivadas