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13-Tert-butoxycarbonylhydrazone of rubomycin was prepared on interaction of rubomycin with tert-butoxycarbonylhydrazine. The new compound showed a high antitumor activity with respect to lymphosarcoma LIO-1 and Garding-Passey melanoma. The compound had no advantages over the initial rubomycin in the treatment of these tumors, was inferior to rubomycin with… (More)
Karminazon (13-benzoylhydrazon) was prepared by condensation of karminomycin with benzoylhydrazine. In its intravenous use in the treatment of mice with lymphosarcoma L10-1 karminazon was less toxic and had lower antitumor activity than karminomycin. Karminazon had a lower selective antitumor activity with respect to lymphosarcoma than karminomycin.
The possibility of chemical modification of carminomycinone-aglycone (II) of carminomicin, a side product in the antibiotic production was studied. The methyl group C-14 was functionilized by introducing the bromine atom and performing a number of exchange reactions with the bromine atom. It was found that under definite conditions (1. 1 equiv. Br2in… (More)
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. The chemotherapeutic… (More)
Doxorubicin and 14-hydroxycarminomycin 14-O-hemiadipates and 14-O-hemipimelates, synthesized from 14-bromo derivatives of daunorubicin and carminomycin and monosodium adipate and pimelate, were converted to the corresponding N-trifluoroacetylated compounds. 13-(4-Methylpiperazine-1-yl)imino derivatives of the anthracycline antibiotics were also obtained.… (More)
A series of phenylthiourea and ethylthiourea derivatives of daunorubicin and its congeners was prepared by reaction of the 3'-amino group of the antibiotic with phenylisothiocyanate or ethylisothiocyanate. S-Methylation yielded S-methylisothiouromium salts which when reacted with amines resulted in an intramolecular cyclization with the participation of the… (More)
Hydrochloride of 14-(I-oxyl-2,2,6,6-tetramethylpiperidyl-4)-acetoxyrubomycin (spin-labeled rubomycin or SL-rubomycin) was prepared by interaction of hydrochloride of 14-bromrubomycin with potassium salt of I-oxyl-2,2,6,6-tetramethylpiperidyl-4-acetic acid. Its interaction with DNA and synthetic poly A and poly U polyribonucleotides was studied. The… (More)
The authors obtained 14-oxykarminomycin by alkaline hydrolysis of 14-bromokarminomycin. On two-fold intravenous administration to mice with lymphosarcoma, strain L10-1, 14-oxycarminomycin showed the same toxicity as karminomycin. The preparation had the same selective antitumor activity as karminomycin.