[Production and antineoplastic activity of new asymmetric azines on the rubomycin base].
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.
Tarasova
V E
VE
Ul'ianova
L A
LA
Iudina
O I
OI
Gol'dberg
L E
LE
Povarov
L S
LS
Olsuf'eva
E N
EN
Bychkova
E N
EN
Shepelevtseva
N G
NG
D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use; D055598:Chemical Phenomena; D002621:Chemistry; D003630:Daunorubicin / Q000138:chemical synthesis* / Q000627:therapeutic use; D004338:Drug Combinations; D004339:Drug Compounding; D004354:Drug Screening Assays, Antitumor; D006835:Hydrazones / Q000138:chemical synthesis* / Q000627:therapeutic use*; D008228:Lymphoma, Non-Hodgkin / Q000188:drug therapy*; D051379:Mice; D014586:USSR
D000970:Antineoplastic Agents; D004338:Drug Combinations; D006835:Hydrazones; D003630:Daunorubicin
Poluchenie i protivoopukholevaia aktivnost' novykh nesimmetrichnykh azinov na osnove rubomitsina.