Abstract

Human topoisomerase II (topoII) enzymes are critical in DNA topology modulation within the cell. Importantly, topoII are validated anticancer drug targets due to their association with cancer cell proliferation. The clinically available topoII targeted anticancer drugs such as etoposide, often show harmful side effects and drug resistance. Therefore, new studies revolving around the design of topoII inhibitors are crucial for the discovery of novel, potent and safer anti-cancer therapeutics. We present an ongoing drug design campaign to optimize compounds centered on a recently patented chemical class of topoIIα inhibitors.

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