Antineoplastic effects of β-carboline derivatives in chronic and acute myeloid leukemia

This study aimed to evaluate the antineoplastic activities of 12 β-carboline derivatives, differing in substituents at the 1- and 3-positions of the β-carboline nucleus, against a panel of leukemia cell lines. We investigated the cytotoxic effects of these derivatives, focusing on their modulation of reactive oxygen species (ROS) generation, autophagy, and key signaling pathways.

Our results demonstrated that β-carboline treatment induced potent, concentration-dependent antineoplastic activity, resulting in significant reductions in cell viability and increased cell death. Importantly, healthy donor mononuclear cells showed limited sensitivity to these compounds. Mechanistic studies revealed that the antineoplastic activity involved the inhibition of ROS production, which subsequently disrupted PI3K/AKT and MAPK/ERK signaling, and the modulation of autophagy processes.