A novel series of α-bromoacryloyl N-substituted isatin analogues 2a-t were found to inhibit the growth and cell viability of human myeloid leukaemia HL-60 and U937 cells as well as human lymphoid leukaemia MOLT-3. Cell death induced by these molecules was preceded by a rapid release of cytochrome c from mitochondria into cytosol and subsequent caspase activation involving caspase-3, to cleave poly (ADP-ribose) polymerase (PARP). These findings suggest that these compounds present antiproliferative activity which may be mediated by apoptosis caused by cytochrome c release and caspase activation in human leukemia cells.
α-Bromoacrylamido N-substituted isatin derivatives as potent apoptosis inducers on human myeloid leukaemia cells
ROMAGNOLI, Romeo;BARALDI, Pier Giovanni;PRETI, Delia;
2009
Abstract
A novel series of α-bromoacryloyl N-substituted isatin analogues 2a-t were found to inhibit the growth and cell viability of human myeloid leukaemia HL-60 and U937 cells as well as human lymphoid leukaemia MOLT-3. Cell death induced by these molecules was preceded by a rapid release of cytochrome c from mitochondria into cytosol and subsequent caspase activation involving caspase-3, to cleave poly (ADP-ribose) polymerase (PARP). These findings suggest that these compounds present antiproliferative activity which may be mediated by apoptosis caused by cytochrome c release and caspase activation in human leukemia cells.File in questo prodotto:
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