[Synthesis and properties of the 14-amino derivatives of daunorubicin and carminomycin].
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.
D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis*; D001407:Bacillus / Q000187:drug effects; D002360:Carubicin / Q000031:analogs & derivatives / Q000032:analysis / Q000138:chemical synthesis*; D003630:Daunorubicin / Q000031:analogs & derivatives* / Q000032:analysis / Q000138:chemical synthesis
D000903:Antibiotics, Antineoplastic; D002360:Carubicin; D003630:Daunorubicin
Sintez i svoĭstva 14-aminoproizvodnykh daunorubitsina i karminomitsina.