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Title: 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 leukaemia cells
Authors: Romagnoli, Romeo
Baraldi, Pier Giovanni
Carrion, Maria Dora
Cruz-Lopez, Olga
Preti, Delia
Tabrizi, Mojgan Aghazadeh
Fruttarolo, Francesca
Heilmann, Jörg
Bermejo, Jaime
Estévez, Francisco 
UNESCO Clasification: 32 Ciencias médicas
320713 Oncología
Keywords: Benzoheterocyclic Derivatives
Anticancer Drugs
Distamycin, et al
Issue Date: 2007
Project: Nuevos Compuestos Antileucémicos 
Journal: Bioorganic and Medicinal Chemistry Letters 
Abstract: 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 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.
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2007.02.048
Source: Bioorganic & Medicinal Chemistry Letters[ISSN 0960-894X],v. 17 (10), p. 2844-2848
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