Discovery of 4-Anilinoquinolinylchalcone Derivatives as Potential NRF2 Activators.

ABSTRACT: Activation of nuclear factor erythroid-2-related factor 2 (NRF2) has been proven to be an effective means to prevent the development of cancer, and natural curcumin stands out as a potent NRF2 activator and cancer chemopreventive agent. In this study, we have synthesized a series of 4-anilinoquinolinylchalcone derivatives, and used a NRF2 promoter-driven firefly luciferase reporter stable cell line, the HaCaT/ARE cells, to screen a panel of these compounds. Among them, (E)-3-{4-[(4-acetylphenyl)amino]quinolin-2-yl}-1-(4-fluorophenyl)prop-2-en-1-one (13b) significantly increased NRF2 activity in the HaCaT cell with a half maximal effective concentration (EC₅₀) value of 1.95 μM. Treatment of compound 13b upregulated HaCaT cell NRF2 expression at the protein le

SUBMITTER: Kao YT 

PROVIDER: S-EPMC7396997 | biostudies-literature | 2020 Jul

REPOSITORIES: biostudies-literature