ANTITUMOR ACTIVITY OF NEW MORPHOLINO ANTHRACYCLINES

Antitumor activity of 3'-deamino-3'-morpholino anthracyclines was examined. Morpholino derivatives of 13-deoxocarminomycins, MX2 (1), MX (2) and MY5 (3) shown in Fig. 1, administered iv showed increase in life span (ILS) values over 110% against ip-inoculated P388 leukemia. The ranges of e...

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Bibliographic Details
Published in:Journal of antibiotics 1988/04/25, Vol.41(4), pp.548-553
Main Authors: KOMESHIMA, NOBUYASU, TSURUO, TAKASHI, UMEZAWA, HAMAO
Format: Article
Language:English
Subjects:
Animals
Antibiotics, Antineoplastic - pharmacology
Antineoplastic agents
Biological and medical sciences
Chemotherapy
Dose-Response Relationship, Drug
Drug Administration Schedule
Female
Leukemia L1210 - drug therapy
Leukemia P388 - drug therapy
Medical sciences
Mice
Naphthacenes - pharmacology
Pharmacology. Drug treatments
Structure-Activity Relationship
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Summary:Antitumor activity of 3'-deamino-3'-morpholino anthracyclines was examined. Morpholino derivatives of 13-deoxocarminomycins, MX2 (1), MX (2) and MY5 (3) shown in Fig. 1, administered iv showed increase in life span (ILS) values over 110% against ip-inoculated P388 leukemia. The ranges of effective doses of these compounds were broader than those of their parent drugs. The morpholino derivatives of doxorubicin and carminomycin, however, were not so effective as their parent drugs. Among these compounds, MX2 administered orally showed nearly the same effects as those obtained by iv administration against P388 leukemia. MX2 administered iv showed 89% ILS against intracerebrally-inoculated L1210 leukemia. The highly lipophilic nature of MX2 could contribute partly to achieving chemotherapeutic responses against intracerebrally-inoculated tumors or by oral administration.
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.41.548