Effects of Methanesulfonic Acid Esters of Aminoglycol on Cultured Ascites Tumor Cells

Abstract

N-Methyl-N, N-bis(3-methylsulfonyloxypropyl)amine 4, 4'-biphenyldisulfonate (838D) and bis(3-methylsulfonyloxypropyl)amine p-toluenesulfonate (864T) are a cross between nitrogen mustard and busulfan. On the cultured Yoshida sarcoma cells, 50% growth inhibition concentration (IC₅₀) of 838D, 864T, and nitrogen mustard was 6.1×10^-3 mM, 1.4×10^-2 mM and 2×10^-5 mM, respectively. Busulfan did not give the value of IC₅₀ in this condition. They were more effective on Yoshida sarcoma and ascites hepatoma AH 13 than on AH 66 or AH 7974. Syntheses of nucleic acid and protein in Yoshida sarcoma cells were not influenced by the addition of 864T or nitrogen mustard at concentrations above IC₅₀. The entry of tumor cells into mitosis was inhibited at the same concentration of these compounds. In the experiments, 864T showed activities similar to that of nitrogen mustard. Characteristic activities of 864T on rats bearing transplantable tumors were not revealed in experiments using cultured tumor cells.