Novel Fluoroquinolone-based Compounds with Anticancer Activity

Dr. Kerns and Dr. Hiasa have discovered novel fluoroquinolones that have anticancer activity. These compounds target type I topoisomerases instead of type II topoisomerases, providing a novel mechanism of action. These compounds inhibit topoisomerase activities without generating double-strand breaks. Thus, the treatment with these compounds is not likely to cause therapy-related acute myeloid leukemia. In vitro tests revealed their significant anti-proliferative activities against many cancer cell lines and an in vivo study showed their efficacy in a colon cancer xenograft model. It is also anticipated that these compounds will be effective against cancers that have developed a resistance to cancer drugs like etoposide. Advantages Target topoisomerase I with a unique mechanism of actionDo not lead to double-strand break generation – better safety profileStrong in vitro data against a wide variety of cancer cell linesPromising in vivo efficacy data in a colon cancer xenograft model.

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