Design, synthesis, and biological evaluation of novel phenol ether derivatives as non-covalent proteasome inhibitors.

ID: ALA4325885

Journal: Eur J Med Chem

Title: Design, synthesis, and biological evaluation of novel phenol ether derivatives as non-covalent proteasome inhibitors.

Authors: Yu J, Xu L, Hong D, Zhang X, Liu J, Li D, Li J, Zhou Y, Liu T.

Abstract: A series of novel phenol ether derivatives were designed, synthesized, and evaluated as non-covalent proteasome inhibitors. Most compounds exhibited moderate to excellent proteasome inhibitory activity. In particular, compound 18x proved to be the most potent compound (chymotrypsin-like: IC₅₀ = 49 nM), exhibiting a 2-fold higher potency compared to the reported PI-1840. Besides, compound 18x exhibited excellent metabolic stability and selective anti-proliferative activity against solid cancer cell lines including HepG2 and HGC27, providing incentive for the further development as a potential anticancer agent against solid cancers.

CiteXplore: 30391816

DOI: 10.1016/j.ejmech.2018.10.056

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