Amonafide

Amonafide is a DNA-intercalating topoisomerase II poison.¹ It reduces the formation of kinetoplast DNA minicircles, a marker of topoisomerase II activity, in a cell-free assay at 100 µM, but does not induce relaxation of supercoiled DNA, a marker of topoisomerase I activity, at the same concentration.² Amonafide inhibits growth in a panel of 11 human cancer cell lines, including leukemia, gastric, breast, and lung cancer cells, with GI₅₀ values ranging from 1 to 10 µM.³ It induces cell cycle arrest at the G₂/M phase and apoptosis in AGS gastric and Huh7 hepatoma cancer cells, respectively, when used at concentrations ranging from 2.5 to 10 µM. Amonafide (5 mg/kg) reduces primary tumor growth and decreases pulmonary metastasis in a murine H22 hepatoma model.⁴

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1. Hsiang, Y.H., Jiang, J.B., and Liu, L.F. Topoisomerase II-mediated DNA cleavage by amonafide and its structural analogs. Mol. Pharmacol. 36(3), 371-376 (1989).

2. Chen, Z., Liang, X., Zhang, H., et al. A new class of naphthalimide-based antitumor agents that inhibit topoisomerase II and induce lysosomal membrane permeabilization and apoptosis. J. Med. Chem. 53(6), 2589-2600 (2010).

3. Liu, Y., Norton, J.T., Witschi, M.A., et al. Methoxyethylamino-numonafide is an efficacious and minimally toxic amonafide derivative in murine models of human cancer. Neoplasia 13(5), 453-460 (2011).

4. Li, M., Wang, Y., Ge, C., et al. Synthesis and biological evaluation of novel alkylated polyamine analogues as potential anticancer agents. Eur. J. Med. Chem. 143, 1732-1743 (2018).