Synthesis and antitumour activity of 4-nitroso-4-(2-chloroethyl)semicarbazides.
1-Methyl-1-(2-chloroethyl)-4-nitroso-4-(2-chloroethyl)semicarbazide, 1,1-di-(2-chloroethyl)-4-nitroso-4-(2-chloroethyl)semicarbazide and 1,1-di-(2-bromoethyl)-4-nitroso-4-(2-chloroethyl)semicarbazide, which are a novel class of nitrosoureas containing hydrazinomustard residue, have been synthesized. A dose-dependent antitumour activity was found with the three tested compounds.
Gugova
R G
RG
Institute of Molecular Biology, Bulgarian Academy of Sciences, Sofia.
Raikov
Z D
ZD
Zakhariev
S G
SG
Demirov
G D
GD
Todorov
D K
DK
Ilarionova
M V
MV
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D007939:Leukemia L1210 / Q000188:drug therapy; D007941:Leukemia P388 / Q000188:drug therapy; D051379:Mice; D008815:Mice, Inbred Strains; D009607:Nitrosourea Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D012663:Semicarbazides / Q000138:chemical synthesis* / Q000494:pharmacology; D014407:Tumor Cells, Cultured / Q000187:drug effects*
D000970:Antineoplastic Agents; D009607:Nitrosourea Compounds; D012663:Semicarbazides; C063657:1,1-di-(2-bromoethyl)-4-nitroso-4-(2-chloroethyl)semicarbazide; C063655:1-methyl-1-(2-chloroethyl)-4-nitroso-4-(2-chloroethyl)semicarbazide; C063656:1,1-di-(2-chloroethyl)-4-nitroso-4-(2-chloroethyl)semicarbazide