Abstract
Rabdosiin ( 1) and its isomer ( 2), isolated from Arnebia euchroma, were potent non-selective inhibitors of mammalian DNA topoisomerases in vitro. Evaluation of synthetic analogs led to the discovery of 3 – 5 as selective inhibitors of topoisomerase II. Unlike etoposide, which inhibits by preventing the DNA rejoining process, compounds 1 – 5 did not induce DNA breakage in either cellular or in vitro assay systems.
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