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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

AuthorsRomagnoli, Romeo; Baraldi, Pier Giovanni; Carrión, María Dora; Cruz-López, Olga; Preti, Delia; Tabrizi, Mojgan Aghazadeh; Fruttarolo, Francesca; Heilmann, Jörg; Bermejo, Jaime ; Estévez, Francisco
Antiproliferative activity
Issue Date25-Feb-2007
CitationBioorganic & Medicinal Chemistry Letters 17(10): 2844-2848 (2007)
AbstractThe 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 α-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 0.24–1.72 μM), significantly superior to that of both alkylating units alone. In human myeloid leukaemia HL-60 cells we observed that these compounds suppress survival and proliferation by triggering morphological changes and internucleosomal DNA fragmentation characteristic of apoptotic cell death. The apoptosis induced by these compounds is mediated by caspase-3 activation and is also associated to an early release of cytochrome c from the mitochondria.
Description5 pages, 4 figures, 1 table.-- PMID: 17346961 [PubMed].-- Printed version published May 15, 2007.
Publisher version (URL)http://dx.doi.org/10.1016/j.bmcl.2007.02.048
Appears in Collections:(IPNA) Artículos
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