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[Synthesis and properties of the 14-amino derivatives of daunorubicin and carminomycin].

作者信息

Povarov L S, Isaeva N N

出版信息

Antibiotiki. 1979 Feb;24(2):92-6.

PMID:434804
Abstract

Interaction of 14-bromine derivatives of daunorubicin and carminomycin, as well as their aglycones with secondary amines, such as piperidine, N-methylpiperazine and morpholine was studied with a purpose of preparing new potentially antitumor antibiotics. It was found that reaction in acetone or dioxan at a temperature of 50--60 degrees C resulted in formation of 14-amino derivatives of the respective bromides. 14-Piperidinyl- and 14-(N-methylpiperazinyl)-daunorubicin, 14-piperidinyl-daunorubicinon and 14-piperidinyl-carminomycinon were prepared. The structure of the new substances was confirmed by the IR, UV and NMR spectra. The antimicrobial activity of 14-amino derivatives amounted to 10--35 per cent of the activity of the initial antibiotics, i.e. daunorubicin and carminomycin.

摘要

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