Mutagenic activity of some newly synthesized cytostatic 1-(2-chloroethyl)-4-arylacyl-1-nitrososemicarbazides in the Salmonella/mammalian microsome assay.

Five experimental anti-leukemic agents, 1-(2-chloroethyl)-4-arylacyl-1-nitrososemicarbazides, were synthesized and tested for genotoxicity in the Salmonella/mammalian microsome assay. No strong mutagenic activity could be detected when tested with the S. typhimurium TA98. A clear dose-dependent base-pair-substitution mutagenic activity was observed with each compound when the tester strain TA100 was used with or without metabolic activation. The genotoxicity of the unsubstituted substance was similar to that of the known mutagenic cytostatic drugs, lomustin and carmustin, and was stronger than the mutagenicity of each substituted derivative.