Synthesis and antitumour activity of several new 4-aroyl-1-nitrosohydrazinecarboxamides.
Six new analogues of nitrosoureas containing aroylhydrazine residue have been synthesized: (I) 4-(2-fluorobenzoyl)-1-(2-chloroethyl)-1-nitrosohydrazinecarboxamide++ +; (II) 4-(4-bromobenzoyl)-1-(2-chloroethyl)-1-nitrosohydrazinecarboxam ide; (III) 4-(4-hydroxybenzoyl)-1-(2-chloroethyl)-1-nitrosohydrazinecarboxamide+ ++; (IV) 4-(3-methoxybenzoyl)-1-(2-chloroethyl)-1-nitrosohydrazinecarbox amide; (V) 4-(4-methoxybenzoyl)-1-(2-chloroethyl)-1-nitrosohydrazinecarbox amide; (VI) 4-(4-fluorophenylacetyl)-1-(2-chloroethyl)-1-nitrosohydrazineca rboxamide. All six compounds showed a dose-dependent in vivo activity against leukaemias L1210 and P388. Compounds I and III were soluble in water. The antitumour effects were highly expressed in compound III, yielding a T/C% value of 402% in leukaemia P388, and in compound VI, 356% in leukaemia L1210.
Gugova
R
R
Institute of Molecular Biology, Bulgarian Academy of Sciences, Sofia, Bulgaria.
Topakbashian
V
V
Lozeva
S
S
Dimov
S
S
Golovinsky
E
E
D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D007939:Leukemia L1210 / Q000188:drug therapy*; D007941:Leukemia P388 / Q000188:drug therapy*; D051379:Mice; D009607:Nitrosourea Compounds / Q000627:therapeutic use*
D000970:Antineoplastic Agents; D009607:Nitrosourea Compounds