Production and antineoplastic activity of new asymmetric azines on the rubomycin base
Tarasova, V.E.; Ul'ianova, L.A.; Iudina, O.I.; Gol'dberg, L.E.; Povarov, L.S.; Olsuf'eva, E.N.; Bychkova, E.N.; Shepelevtseva, N.G.
Antibiotiki i Khimioterapiia 35(4): 21-24
1990
ISSN/ISBN: 0235-2990 PMID: 2383140 Document Number: 359903
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.