Bicyclic Cyclohexenones as Inhibitors of NF-κB Signaling | Zendy

Joseph K. Hexum | Zendy; Rodolfo TelloAburto | Zendy; Nicholas B. Struntz | Zendy; Andrew M. Harned | Zendy; Daniel A. Harki | Zendy

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Bicyclic Cyclohexenones as Inhibitors of NF-κB Signaling

Author(s) -

Joseph K. Hexum,

Rodolfo TelloAburto,

Nicholas B. Struntz,

Andrew M. Harned,

Daniel A. Harki

Publication year - 2012

Publication title -

acs medicinal chemistry letters

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.065

H-Index - 66

ISSN - 1948-5875

DOI - 10.1021/ml300034a

Subject(s) - bicyclic molecule , p50 , chemistry , nf κb , covalent bond , stereochemistry , signal transduction , inhibitory postsynaptic potential , biochemistry , combinatorial chemistry , biology , transcription factor , gene , organic chemistry , neuroscience

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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