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Updated: May 19, 2026

Synthesis and Characterization of an Aspirin-fumarate Prodrug that Inhibits NFκB Activity and Breast Cancer Stem Cells
Published on: January 18, 2017
Bicyclic Cyclohexenones as Inhibitors of NF-κB Signaling
Joseph K Hexum1, Rodolfo Tello-Aburto, Nicholas B Struntz
1Department of Medicinal Chemistry, University of Minnesota, 717 Delaware St SE, Minneapolis, MN, 55414, USA.
Abstract:
A series of structurally simplified cryptocaryone analogues were synthesized by a facile Pd-catalyzed acetoxylation of alkyne-tethered cyclohexadienones and evaluated as inhibitors of NF-κB signaling. Compounds 10 and 11 were found to possess low micromolar inhibitory properties towards induced NF-κB activity by blocking p50/p65 nuclear protein through a covalent inhibition mechanism. Both compounds were able to inhibit NF-κB-induced IL-8 expression and exhibited antiproliferative activity against two model cancer cell lines. These analogues constitute a promising new scaffold for the development of novel NF-κB inhibitors and anticancer agents.
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