[Production and antineoplastic activity of new asymmetric azines on the rubomycin base]

Antibiot Khimioter. 1990 Apr;35(4):21-4.
[Article in Russian]

Abstract

New alkulidene hydrazones of rubomycin (daunorubicin) with the linear or branched chain of the carbon atoms were studied: rubomycin 13-(hexylidene-2")-hydrazone, rubomycin 13-(heptylidene-3")-hydrazone and rubomycin 13-(4"-methylpentylidene-2")-hydrazone. Alkylidene hydrazones of the formamidine derivatives were also studied: 13:cyclohexylidene hydrazone of 3'-desamino-3'-dimethylformamidine rubomycin and 13-(5"-oxypentyliden-2") hudrazone of 3'-desamino-3'-dimethylformamidine rubomycin. The latter two alkylidene hydrazones were modified twice. It was found that after a single intravenous administration to tumor-free mice the new substance had the same or lower toxicity as compared to that of rubomycin. Antitumor activity of the substances against lymphosarcoma LIO-I was studied comparatively with that of the initial rubomycin. It was shown that the molecule modification at C-13, as well as simultaneous modification at C-13 and the sugar amino group resulted in lowering of the antitumor activity in comparison to that of the starting rubomycin.

Publication types

  • Comparative Study
  • English Abstract

MeSH terms

  • Animals
  • Antineoplastic Agents / therapeutic use
  • Chemical Phenomena
  • Chemistry
  • Daunorubicin / chemical synthesis*
  • Daunorubicin / therapeutic use
  • Drug Combinations
  • Drug Compounding
  • Drug Screening Assays, Antitumor
  • Hydrazones / chemical synthesis*
  • Hydrazones / therapeutic use*
  • Lymphoma, Non-Hodgkin / drug therapy*
  • Mice
  • USSR

Substances

  • Antineoplastic Agents
  • Drug Combinations
  • Hydrazones
  • Daunorubicin