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Fluorinated Anthracyclines: Synthesis and Biological Activity

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Organic structures with fluorine atom are slightly diffuse in nature.

Starting '80s researchers have discovered that the selective introduction of fluorine into biologically active molecules exercised an influence on activity. So an important endeavour in drug design have been described and numerous compounds incorporating fluorine as either a bioisosteric replacement for hydrogen or an isoelectronic replacement for the hydroxyl group have been reported.

Parallely, an enormous literature on anthracyclines exists, a class of compounds used in clinical since '70s, as antitumor drugs. Unfortunately, the anthracyclines are known as well for several toxical effects that frequently condition the clinical use.

In the last decade a lot of anthracycline derivatives has been described in which has been introduced a fluorine atom in different position of molecule.

This review wishes to represent an updated collection of compounds with anthracycline structure where a fluorine atom has been introduced on aglycon or / and sugar moiety.

Together with the chemical structures, the synthetic indications are furnished and succinct explanations of biological activity are summarised (if available).

Keywords: DAUNO derivatives; Fluorinated Anthracyclines; IDARUBICIN; Multidrug Resistance (MDR); OXYAGLYCONE; demethoxydaunorubicin; eukaryotic topoisomerase

Document Type: Review Article


Publication date: 2002-03-01

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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