N-salicylidene derivatives of pirarubicin.
The preparation and biological evaluation of N-salicylidene derivatives of pirarubicin are described. Pirarubicin was treated with various kinds of aryl aldehydes. Most of compounds synthesized here were more active than pirarubicin in vitro. Some of them showed significant prolongation of the survival period in experimental mice by oral administration. Interestingly, a derivative containing forphenicine exhibited the broadest dose-response range by intraperitoneal administration.
Ajito
K
K
Institute of Microbial Chemistry, Tokyo, Japan.
Ikeda
D
D
Komuro
K
K
Nosaka
C
C
Wako
N
N
Kondo
S
S
Takeuchi
T
T
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage / Q000138:chemical synthesis / Q000627:therapeutic use*; D055598:Chemical Phenomena; D002621:Chemistry; D002855:Chromatography, Thin Layer; D004305:Dose-Response Relationship, Drug; D004317:Doxorubicin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000627:therapeutic use; D005260:Female; D007939:Leukemia L1210 / Q000188:drug therapy*; D007941:Leukemia P388 / Q000188:drug therapy*; D007942:Leukemia, Experimental / Q000188:drug therapy*; D051379:Mice; D015394:Molecular Structure; D014407:Tumor Cells, Cultured
D000903:Antibiotics, Antineoplastic; D004317:Doxorubicin; C027260:pirarubicin