Unknown

Dataset Information

0

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 |

REPOSITORIES: biostudies-literature

Similar Datasets

| S-EPMC3193406 | biostudies-other
| S-EPMC8867604 | biostudies-literature
| S-EPMC3044936 | biostudies-literature
| S-EPMC3075605 | biostudies-other
| S-EPMC8706767 | biostudies-literature
| S-EPMC4683373 | biostudies-other
| S-EPMC8639591 | biostudies-literature
2023-05-10 | PXD039305 | Pride
| S-EPMC3532050 | biostudies-other
| S-EPMC5485221 | biostudies-literature