A novel series of alpha-bromoacryloyl N-substituted isatin analogues were found to inhibit the growth and viability of human myeloid leukemia HL-60 and U-937 cells as well as human lymphoid leukemia MOLT-3 cells. Cell death induced by these molecules was preceded by a rapid release of cytochrome c from mitochondria into the 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.
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