Povarov L S, Leont'eva O V, Bernaki P D, Olsuf'eva E N, Salimova E I, Pera P, Preobrazhenskaia M N
Grace Cancer Drug Center, Roswell Park Cancer Institute, Buffalo, New York, USA.
Bioorg Khim. 1995 Dec;21(12):925-32.
Doxorubicin and 14-hydroxycarminomycin 14-O-hemiadipates and 14-O-hemipimelates, synthesized from 14-bromo derivatives of daunorubicin and carminomycin and monosodium adipate and pimelate, were converted to the corresponding N-trifluoroacetylated compounds. 13-(4-Methylpiperazine-1-yl)imino derivatives of the anthracycline antibiotics were also obtained. The cytostatic activity of the compounds synthesized was studied using a panel of human and animal tumor cell lines sensitive or resistant to doxorubicin. N-Trifluoroacetylation of the antibiotics resulted in a decrease in the cytostatic activity. The activity of the water-soluble 13-(4-methylpiperazine-l-yl)imino derivatives is close to that of the corresponding parent antibiotics.
由柔红霉素和洋红霉素的14-溴衍生物与己二酸钠和庚二酸钠合成的阿霉素以及14-羟基洋红霉素14-O-半己二酸酯和14-O-半庚二酸酯被转化为相应的N-三氟乙酰化化合物。还获得了蒽环类抗生素的13-(4-甲基哌嗪-1-基)亚氨基衍生物。使用一组对阿霉素敏感或耐药的人和动物肿瘤细胞系研究了合成化合物的细胞抑制活性。抗生素的N-三氟乙酰化导致细胞抑制活性降低。水溶性13-(4-甲基哌嗪-1-基)亚氨基衍生物的活性与相应的母体抗生素相近。