The Ohio State University

Edgar S Diaz-Cruz

Robert Brueggemeier

Bin Su

Serena Landini

Compounds and methods suppressing aromatase activity expression in cancer cells. Provided are compounds are those of formula I: wherein Rmay be alkyl, cycloalkyl, haloalkyl, aryl, substituted aryl, haloaryl, alkoxy, alkylaryl, and arylalkyl; Ris H, alkyl, aryl, alkylaryl, arylalkyl, and cycloalkyl; R, with the base nitrogen, forms an amide or sulfonamide; Ris selected from nitro, amine, amide, and benzamide; or a pharmaceutically acceptable salts thereof. Also provided are small molecule selective aromatase inhibitors having a molecular weight of less 500 g/mol. In some embodiments, the small molecule selective aromatase inhibitors described herein have a molecular weight of less than 450 g/mol. Also provided are methods for suppressing aromatase activity expression in cancer cells comprising the step of administering a pharmaceutically effective amount of a small molecule aromatase inhibitor to a subject in need of such treatment. In one embodiment, the cancer cells are breast cancer cells.

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Columbus, OH, United States of America

Edgar S Diaz-Cruz