[Chemical modification of an antineoplastic antibiotic bleomycetin by the C-end fragment].

Bleomycetin, an antitumor antibiotic, was subjected to chemical modification by the C-end fragment i.e. the residue of 3-[(4-aminobutyl)amino]propylamine (spermidine++) with acylation, carbamoylation and reducing alkylation, which yielded its new semisynthetic derivatives.

[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.

[Study of toxicity and antineoplastic activity of 14-substituted derivatives of rubomycin and carminomycin].

Toxicity and antitumor activity of five derivatives of rubomycin and carminomycin were studied in animals. The derivatives were prepared by modification of the methyl C-14 group. These were the following: 14-chlorrubomycin, 14-chlorcarminomycin, 14-salicyloyloxyrubomycin, 14-salicyloyloxycarminomycin and 14-quinaldinoyloxyrubomycin.

[Glycopeptide antibiotics: eremomycin, vancomycin, and teicoplanin. Comparison of several parameters of pharmacokinetics and antimicrobial activity].

Pharmacokinetic parameters of eremomycin (Institute of New Antibiotics, the USSR Academy of Medical Sciences), teichoplanin (Lepetit) and vancomycin (Eli Lilly) were compared after their intravenous administration to rats in the same dose of 50 mg/kg. It was shown that the area under the concentration time curve of eremomycin was 2 times smaller than that of teichoplanin and 6 times larger than that of vancomycin. The mean retention time of eremomycin was close to that of teichoplanin and 1.

[Eremomycin--a new antibiotic of the polycyclic glycopeptide group].

Eremomycin is a novel antibacterial antibiotic. It was isolated at the Institute of New Antibiotics, the USSR Academy of Medical Sciences from the culture fluid of actinomycete INA-238. By its physico-chemical and biological properties the antibiotic was classified as belonging to the group of polycyclic glycopeptides.