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

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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

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

doi

10.1016/j.ejmech.2018.02.073

subject

Has Abstract

pub_date

2018-04-10 00:00:00

pages

90-97

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(18)30210-1

journal_volume

149

pub_type

杂志文章

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