Design, synthesis, and evaluation of asymmetric EF24 analogues as potential anti-cancer agents for lung cancer.
Basic Information
ID: ALA4041523
Journal: Eur J Med Chem
Title: Design, synthesis, and evaluation of asymmetric EF24 analogues as potential anti-cancer agents for lung cancer.
Authors: Wu J, Wu S, Shi L, Zhang S, Ren J, Yao S, Yun D, Huang L, Wang J, Li W, Wu X, Qiu P, Liang G.
Abstract: The nuclear factor-kappa B (NF-κB) signaling pathway has been targeted for the therapy of various cancers, including lung cancer. EF24 was considered as a potent inhibitor of NF-κB signaling pathway. In this study, a series of asymmetric EF24 analogues were synthesized and evaluated for their anti-cancer activity against three lung cancer cell lines (A549, LLC, H1650). Most of the compounds exhibited good anti-tumor activity. Among them, compound 81 showed greater cytotoxicity than EF24. Compound 81 also possessed a potent anti-migration and anti-proliferative ability against A549 cells in a concentration-dependent manner. Moreover, compound 81 induced lung cancer cells death by inhibiting NF-κB signaling pathway, and activated the JNK-mitochondrial apoptotic pathway by increasing reactive oxygen species (ROS) generation resulting in apoptosis. In summary, compound 81 is a valuable candidate for anti-lung cancer therapy.
CiteXplore: 27886548
DOI: 10.1016/j.ejmech.2016.10.027
Patent ID: ┄