SYNTHESIS AND ANTITUMOR-ACTIVITY OF SEVERAL NEW 4-AROYL-1-NITROSOHYDRAZINECARBOXAMIDES

Six new analogues of nitrosoureas containing aroylhydrazine residue ha ve been synthesized: (1) )-1-(2-chloroethyl)-1-nitrosohydrazinecarboxa mide; (II) )-1-(2-chloroethyl)-1-nitrosohydrazinecarboxamide; (III) )- 1-(2-chloroethyl)-1-nitrosohydrazinecarboxamide; (IV) )-1-(2-chloroeth yl)-1-nitrosohyorazinecarboxamide; (V) )-1-(2-chloroethyl)-1-nitrosohy drazinecarboxamide; (VI) 4-(4-fluorophenylacetyl)-1-(2-chloroethyl)-1 -nitrosohydrazinecarboxamide. All six compounds showed a dose-dependen t 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.