Synthesis and Evaluation of NF-κB Inhibitory Activity of Mollugin Derivatives.

ABSTRACT: (1) Background: Nuclear factor κB (NF-κB) is an important transcriptional regulator that regulates the inflammatory pathway and plays a key role in cellular inflammatory and immune responses. The presence of a high concentration of NF-κB is positively correlated with the severity of inflammation. Therefore, the inhibition of this pathway is an important therapeutic target for the treatment of various types of inflammation; (2) Methods: we designed and synthesized 23 mollugin derivatives and evaluated their inhibitory activity against NF-κB transcription; (3) Results: Compound 6d exhibited the most promising inhibitory activity (IC₅₀ = 3.81 µM) and did not show any significant cytotoxicity against the tested cell lines. Investigation of the mechanism of action indicated th

SUBMITTER: Zhang LH 

PROVIDER: S-EPMC9695821 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature