Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10591063 | Bioorganic & Medicinal Chemistry Letters | 2014 | 7 Pages |
Abstract
A series of cinnamylideneacetophenones were synthesized via a modified Claisen-Schmidt condensation reaction and evaluated for cytotoxicity against breast cancer cells using the Alamar Blue⢠assay. Derivatives 17 and 18 bearing a 2-nitro group on the B ring, exhibited sub-micromolar cytotoxicity in MCF-7 cells (IC50 = 71 and 1.9 nM), respectively. Derivative 17 also displayed sub-micromolar (IC50 = 780 nM) cytotoxicity in MDA-MB-468 cells. Additionally, 17 and 18 displayed significantly less cytotoxicity than the chemotherapeutic doxorubicin in non-tumorigenic MCF-10A cells. This study provides evidence supporting the continued development of nitro-substituted cinnamylideneacetophenones as small molecules to treat breast cancer.
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Authors
David J. Weldon, Marilyn D. Saulsbury, Joshua Goh, Leah Rowland, Petreena Campbell, Laijia Robinson, Calvin Miller, Joshua Christian, Louisa Amis, Nia Taylor, Cassandra Dill, Willie Jr., Stanley L. Evans, Eileen Brantley,