Document Report Card

Basic Information

ID: ALA4196055

Journal: Eur J Med Chem

Title: Synthesis and biological evaluation of α-santonin derivatives as anti-hepatoma agents.

Authors: Chen H, Yang X, Yu Z, Cheng Z, Yuan H, Zhao Z, Wu G, Xie N, Yuan X, Sun Q, Zhang W.

Abstract: A series of α-santonin-derived compounds as potentially anti-hepatoma agents were designed and synthesized in an effort to find novel therapeutic agents. Among them, derivative 5h was more potent than the positive control 5-fluorouracil (5-Fu) on HepG-2, QGY-7703 and SMMC-7721 with IC50 values of 7.51, 3.06 and 4.08 μM, respectively. The structure-activity relationships (SARs) of these derivatives were discussed. In addition, flow cytometry and western blot assay revealed that the derivatives induced hepatoma cells apoptosis by facilitating apoptosis-related proteins expressions. Our findings suggested that these α-santonin-derived analogues hold promise as chemotherapeutic agents for the treatment of human hepatocellular cancer.

CiteXplore: 29499490

DOI: 10.1016/j.ejmech.2018.02.073