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-nitrosohydrazinecarboxamide; (III) 4-(4-hydroxybenzoyl)-1-(2-chloroethyl)-1-nitrosohydra-zinecarboxamide; (IV) 4-(3-methoxybenzoyl)-1-(2-chloroethyl)-1-nitrosohydrazinecarboxamide; (V) 4-(4-methoxybenzoyl)-1-(2-chloroethyl)-1-nitrosohydrazinecarboxamide; (VI) 4-(4-fluorophenylacetyl)- 1-(2-chloroethyl)-1-nitrosohydrazinecarboxamide. All six compounds showed a dose-dependent in vivo activity against leukaemias L 1210 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 L 1210.