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Bicyclic Cyclohexenones as Inhibitors of NF-κB Signaling.

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.

SUBMITTER: Hexum JK 

PROVIDER: S-EPMC3409840 | biostudies-literature | 2012 Jun

REPOSITORIES: biostudies-literature

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Bicyclic Cyclohexenones as Inhibitors of NF-κB Signaling.

Hexum Joseph K JK   Tello-Aburto Rodolfo R   Struntz Nicholas B NB   Harned Andrew M AM   Harki Daniel A DA  

ACS medicinal chemistry letters 20120511 6

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 again  ...[more]

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