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

Romagnoli, Romeo ; Baraldi, Pier Giovanni ; Carrion, Maria Dora ; Cruz-Lopez, Olga ; Preti, Delia ; Tabrizi, Mojgan Aghazadeh ; Fruttarolo, Francesca ; Heilmann, Jörg ; Bermejo, Jaime ; Estevez, Francisco



Abstract

The synthesis and biol. activity of a series of hybrids I (n = 3, 6; X = NH, NMe, O, S) prepd. 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 compds. were highly cytotoxic against the human myeloid leukemia cell lines HL-60 and ...

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