Genotoxic effect of 4-aroyl-1-(2-chloroethyl)-1nitrosohydrazinecarboxamides on Saccharomyces cerevisiae cells.
The study of some 4-aroyl-1-(2-chloroethyl)-1-nitrosohydrazinecarboxamides with a Saccharomyces cerevisiae mutagenicity test of increased sensitivity defined two of them, 4-(4-bromobenzoyl)-1-(2-chloroethyl)-1-nitrosohydrazinecarboxam ide and 4-(4-fluorophenyl)-1-(2-chloroethyl)-1-nitrosohydrazine carboxamide as typical cytostatic agents. At concentrations of 2-5 microg/ml the substances kill up to 60%-70% of cells without having any detectable recombinogenic and mutagenic effects. At the same concentrations, lomustine, well known as a cytostatic reference, demonstrated recombinogenic and mutagenic activity on yeast cells. The advantage of the newly synthesized substances is that, in a certain concentration range, their biological activity is mainly cytotoxic without induction of recombinogenic and mutagenic events in surviving cells.
Staleva
L
L
Institute of Molecular Biology, Bulgarian Academy of Sciences, Sofia. liliana@obzor.bio21.acad.bg
Gugova
R
R
Venkov
P
P
Waltscheva
L
L
Golovinsky
E
E
D000970:Antineoplastic Agents / Q000633:toxicity*; D002330:Carmustine / Q000031:analogs & derivatives; D006834:Hydrazines / Q000633:toxicity; D008130:Lomustine / Q000031:analogs & derivatives; D009152:Mutagenicity Tests; D009607:Nitrosourea Compounds / Q000633:toxicity*; D012441:Saccharomyces cerevisiae / Q000187:drug effects* / Q000235:genetics*
C113631:4-(4-bromobenzoyl)-1-(2-chloroethyl)-1-nitrosohydrazinecarboxamide; C113632:4-(4-fluorophenyl)-1-(2-chloroethyl)-1-nitrosohydrazinecarboxamide; D000970:Antineoplastic Agents; D006834:Hydrazines; D009607:Nitrosourea Compounds; D008130:Lomustine; D002330:Carmustine