Golovinsky E, Gugova R, Norpoth K, Mohtashamipur E
Institute of Molecular Biology, Bulgarian Academy of Sciences, Sofia.
J Cancer Res Clin Oncol. 1991;117(1):1-3. doi: 10.1007/BF01613187.
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.
合成了五种实验性抗白血病药物，即1-(2-氯乙基)-4-芳酰基-1-亚硝基氨基脲，并在沙门氏菌/哺乳动物微粒体试验中对其遗传毒性进行了测试。用鼠伤寒沙门氏菌TA98进行测试时，未检测到强烈的诱变活性。当使用测试菌株TA100并进行或不进行代谢活化时，每种化合物均观察到明显的剂量依赖性碱基对替代诱变活性。未取代物质的遗传毒性与已知的诱变细胞抑制药物洛莫司汀和卡莫司汀相似，且比每种取代衍生物的诱变性更强。
