[Antineoplastic activity and toxicity of dihydroambazone in comparison with ambazone (1,4-benzoquinone-guanylhydrazone-thiosemicarbazone)].

Abstract

Dihydroambazone 1, a soluble derivative of ambazone, was tested with an admixture of ascorbic acid (0.1, 0.25, or 0.5% in distilled water) for antineoplastic activity by different routes (i.p., p.o., s.c., i.v.) against leukemia P388, and by s.c. application against Lewis lung carcinoma on B6D2F1-mice. The results were compared with that of ambazone. 1 was as active as ambazone upon the per os d 1-4 schedule only. Ascorbic acid, added for stabilization of 1, had no significant influence on the results. Intravenously given 1 was of low activity. It proved to be toxic at 100 mg/kg body mass. The i.v. toxicity was estimated approximately on B6D2F1-mice (LD50: 150 mg/kg; LD100: 175 mg/kg; maximum tolerated dose (MTD): 100 mg/kg. A comparison between the MTD's of 1 and ambazone in mice and rats (Wistar) showed partly a somewhat better p.o. compatibility of 1. The expectation of a favourable i.v. applicable derivative from the otherwise in water nearly insoluble ambazone could not be realized.

• Authors: W Gutsche, A Härtl, J Baumgart, W Schulze
• Journal: Die Pharmazie (Pharmazie) Vol. 45 Issue 1 Pg. 55-7 (Jan 1990) ISSN: 0031-7144 [Print] Germany
• Vernacular Title: Antineoplastische Wirksamkeit und Toxizität von Dihydroambazon im Vergleich zu Ambazon (1,4-Benzochinon-guanylhydrazon-thiosemicarbazon).
• PMID: 2333315 (Publication Type: Comparative Study, English Abstract, Journal Article)

Chemical References

• Antineoplastic Agents
• dihydroambazone
• 1,4-benzoquinone guanylhydrazone thiosemicarbazone
• Mitoguazone

Topics

• Animals
• Antineoplastic Agents
• Lethal Dose 50
• Leukemia P388 (drug therapy)
• Mice
• Mice, Inbred C57BL
• Mice, Inbred DBA
• Mice, Inbred Strains
• Mitoguazone (analogs & derivatives, pharmacology, toxicity)
• Rats
• Rats, Inbred Strains