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Synthesis and Biological Evaluation of α-santonin Derivatives as Anti-Hepatoma Agents

Hao Chen, Xiao Yang, Zongmin Yu, Ziying Cheng, Hu Yuan, Zeng Zhao, Guozhen Wu, Ning Xie, Xing Yuan, Qingyan Sun, Weidong Zhang

Eur J Med Chem. 2018 Apr 10;149:90-97.

PMID: 29499490

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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP481061 α-Santonin α-Santonin 481-06-1 Price
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