β-carboline-ACS81 is a potent antitumor β-carboline derivative. It induces apoptosis in HL-60 cells by causing mitochondrial membrane potential collapse and arrests the cell cycle at the G2/M phase. This compound exhibits significant antiproliferative activity against HL-60 cells (IC50 = 1.52 μM). β-carboline-ACS81 is applicable for research in leukemia, histiocytic lymphoma, hepatocellular carcinoma, malignant melanoma, colorectal cancer, and lung cancer.

β-Carboline-ACS81 (Compound 12c) exhibits significant antiproliferative activity against various tumor cell lines within 72 hours, with IC50 values for HL-60, U937, HepG2, HCT-116, A375, and A549 cells at 1.52, 2.03, 2.8, 6.04, 6.57, and 37.23 μM, respectively, while the IC50 value for normal L-02 cells is 33.92 μM. Additionally, β-carboline-ACS81 (0.38-1.52 μM, 48 hours) can induce cell cycle arrest at the G2/M phase in HL-60 cells, thereby inhibiting proliferation and triggering apoptosis, possibly mediated by the mitochondrial pathway, as indicated by the reduction in mitochondrial membrane potential.