Hybrid molecules containing benzo[4,5]imidazo[1,2-d][1,2,4]thiadiazole and α-bromoacryloyl moieties as potent apoptosis inducers on human myeloid leukaemia cells

Romagnoli, Romeo ; Baraldi, Pier Giovanni ; Carrion, Maria Dora

; Cruz-Lopez, Olga ; Preti, Delia ; Tabrizi, Mojgan Aghazadeh ; Fruttarolo, Francesca ; Heilmann, Jörg ; Bermejo, Jaime ; Estévez, Francisco

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Zusammenfassung

The synthesis and biological activity of a series of hybrids 1-5 prepared combining a benzo[4,5]imidazo[1,2-d][1,2,4]thiadiazole and different benzoheterocyclic alpha-bromoacryloyl amides have been described and their structure-activity relationships discussed. All these hetero-bifunctional compounds were highly cytotoxic against the human myeloid leukaemia cell lines HL-60 and U937 (IC50 ...