Topoisomerase II Inhibitors

7.05.3.1 Anthracyclines

The great clinical success of the anthracycline doxorubin (12)70 has ensured that a large effort has been put into other anthracycline analogs. Among the goals of this research has been to lower the cumulative cardiotoxicity seen with this drug, and also to develop semisynthetic or wholly synthetic analogs. Several such new anthracycline derivatives are reported on here.

Another, broader goal for improving all classes of DNA-intercalating topo II agents is to decrease their susceptibility to cell efflux pumps such as P-gp, and this is a second broad theme. However, the search for new topo II agents is not restricted to anthracyclines, or even to DNA intercalators, with a wide variety of both synthetic and natural product structures under development.

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