Influence of the Structure of New Anthracycline Antibiotics on their Biological Properties

In the search for new derivatives of anthracycline antibiotics with advantageous biological properties, particularly with lower toxicity and/or higher activity, a series of new analogs of antibiotics applied in therapy such as daunorubicin, doxorubicin, as well as epidoxorubicin and, for comparison,...

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Bibliographic Details
Published in:Anticancer research 2005-05, Vol.25 (3B), p.2043-2048
Main Authors: WASOWSKA, Malgorzata, OSZCZAPOWICZ, Irena, WIETRZYK, Joanna, OPOLSKI, Adam, MADEJ, Janusz, DZIMIRA, Stanislaw, OSZCZAPOWICZ, Janusz
Format: Article
Language:English
Subjects:
Animals
Anthracyclines - chemical synthesis
Anthracyclines - chemistry
Anthracyclines - pharmacology
Anthracyclines - toxicity
Antibiotics, Antineoplastic - chemical synthesis
Antibiotics, Antineoplastic - chemistry
Antibiotics, Antineoplastic - pharmacology
Antibiotics, Antineoplastic - toxicity
Biological and medical sciences
Cell Line, Tumor
Daunorubicin - analogs & derivatives
Daunorubicin - chemical synthesis
Daunorubicin - chemistry
Daunorubicin - pharmacology
Daunorubicin - toxicity
Doxorubicin - analogs & derivatives
Drug Screening Assays, Antitumor
Epirubicin - analogs & derivatives
Heart Diseases - chemically induced
Humans
Male
Medical sciences
Mice
Mice, Inbred BALB C
Mice, Inbred DBA
Structure-Activity Relationship
Tumors
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Summary:In the search for new derivatives of anthracycline antibiotics with advantageous biological properties, particularly with lower toxicity and/or higher activity, a series of new analogs of antibiotics applied in therapy such as daunorubicin, doxorubicin, as well as epidoxorubicin and, for comparison, analogs of epidaunorubicin, have been synthesized. Our results show that the new derivatives have antiproliferative activities similar to or higher than the parent antibiotics. The toxicities of these analogs were significantly lower, with LD 50 values from 1.8- to 18.4-fold higher than the referential drugs. Cardiotoxicity determinations, using male mice treated with a single dose of 75% of the LD 50 values of all tested compounds, indicated that the cardiotoxicity of the new analogs is significantly lower than that of the parent drugs.
ISSN:0250-7005
1791-7530