L. S. Povarov

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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)
Natural anthracycline antibiotics, such as daunorubicin, doxorubicin, carminomycin, and aclacinomycin are important agents in chemotherapy of tumor diseases. As the result of extensive research carried out on their chemical modification, several semisynthetic anthracycline preparations have been obtained having enhanced antitumor action. Of greatest(More)
Streptomyces grisoruber strain 1618-306 produces three types of anthracycline antibiotics, derivatives of epsilon-pyrromycinone (methyl (7S, 9R, 10R)-9-ethyl-5,7,8,9,10,12-hexahydro-1,4,6,7,9-pentahydroxy-5,12-di oxo-10- naphthacenecarboxylate), epsilon-1-hydroxyauramycinone and epsilon-1-hydroxysulfurmycinone, differing in C-9 substituent in D ring of(More)
Derivatives of antitumour anthracycline antibiotics containing N-methylurea moiety in the carbohydrate ring were obtained by the interaction of methyl isocyanate with daunorubicin, doxorubicin, carminomycin and daunorubicin derivatives, substituted at C-13 or C-14 positions. N-Nitrosation of these compounds yielded modified anthracycline antibiotics(More)
USSR Inventor's Certificate No. 511,324, Otkrytiya, No. 15 (1976). Yu. P. Vainberg, L. V. Egorov, L. B. Shagalov, et al., Khim.-farm. Zh., No. 9, 18-22 (1980). Yu. P. Vainberg, L. B. Shagalov, and S. V. Pinevich, Khim.-farm. Zh., No. 9, 10511054 (1985). Yu. P. Vainberg, L. B. Shagalov, E. I. Yartsev, and G. N. Loginova, Khim.-farm. Zh., No. 5, 577-579(More)
Synthesis of 2 new N-acyl derivatives of carminomycin and rubomycin (N-L-leucylcarminomycin and N-sarcolysylrubomycin) is described. Acute toxicity of the new and 4 known N-acyl derivatives: N-acetylcarminomycin, N,L-alanylcarminomycin, N-D-phenylalanylcarminomycin and N-D-phenylalanylrubomycin was studied on albino mice. It was shown that the N-acyl(More)
A dihydro derivative of karminomycin was prepared using chemical reduction with potassium boron hydride. When dihydrokarminomycin was administered intravenously to healthy albino mice in a single dose it practically showed the same toxicity as karminomycin. However, unlike the latter dihydrokarminomycin induced the death of the animals at later periods of(More)
13-Tret-butoxycarbonyl hydrazone (BOC hydrazone) of carminomycin was prepared by interaction of carminomycin with tret-butoxycarbonyl hydrazine. Interaction of carminomycin with N-amino-N'-methyl piperazine resulted in 13-(4-methyl piperazinyl) imine (MP imine) of carminomycin. BOC hydrazone and MP imine of carminomycin had a significant antiblastomic(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.