Benzisothiazole: A Novel Class of Carbonyl Reductase Inhibitors

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Student Presentation

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Faculty Sponsor

Henry Charlier


Anthracyclines are commonly used chemotherapy drugs in the treatment of cancer. However, anthracycline use is linked a potentially lethal cardiotoxicity. Carbonyl reductase is an enzyme that catalyzes the reduction of anthracyclines to their alcohol metabolites. These metabolites have been shown to be a significant contributor to the cardiotoxicity. Therefore controlling the rate of anthracycline reduction by carbonyl reductase may be useful in lowering the risk of heart damage during cancer treatment. Studies were done to identify potential carbonyl reductase inhibitors that could be used to block the reduction of the anthracyclines, thereby preventing the formation of the cardiotoxic metabolites. One such compound was 1,2-benzisothiazole. This compound was determined to be a modest inhibitor the enzyme. Although this compound is not a good drug candidate, it does reveal another potential class of compounds to investigate as inhibitor candidates.

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