Synthesis and antileukemic activity of N-enamine derivatives of daunorubicin, 5-iminodaunorubicin, and doxorubicin.
Eleven N-enamine derivatives of daunorubicin and of its 5-imino analogue as well as of doxorubicin have been synthesized and evaluated for antileukemic activity in vitro and in vivo. Comparison of biological activities of examined compounds with other enamine derivatives of daunorubicin, reported earlier by us, has indicated that the optimal activity is shown by N-(1-carboethoxypropen-1-yl-2)daunorubicin.
Stefańska
B
B
Department of Pharmaceutical Technology and Biochemistry, Technical University of Gdańsk, Poland.
Dzieduszycka
M
M
Bontemps-Gracz
M
M
Borowski
E
E
Martelli
S
S
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis* / Q000627:therapeutic use; D003630:Daunorubicin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000627:therapeutic use; D004317:Doxorubicin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000627:therapeutic use; D004354:Drug Screening Assays, Antitumor; D007274:Injections, Intraperitoneal; D007939:Leukemia L1210 / Q000188:drug therapy; D007941:Leukemia P388 / Q000188:drug therapy; D051379:Mice; D013329:Structure-Activity Relationship
D000903:Antibiotics, Antineoplastic; D004317:Doxorubicin; C055557:N-(1-carboethoxylpropen-1-y-2)daunorubicin; D003630:Daunorubicin