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International Journal of Molecular Medicine
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February 2013 Volume 31 Issue 2

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International Journal of Molecular Medicine is an international journal devoted to molecular mechanisms of human disease.

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Experimental and Therapeutic Medicine is an international journal devoted to laboratory and clinical medicine.

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Article

Novel rotundic acid derivatives: Synthesis, structural characterization and in vitro antitumor activity

  • Authors:
    • Yu Chen
    • Yu-Fang He
    • Min-Lun Nan
    • Wen-Yi Sun
    • Jie Hu
    • Ai Cui
    • Fan Li
    • Fang Wang
  • View Affiliations / Copyright

    Affiliations: Department of Pathogenobiology, Norman Bethune College of Medicine, Jilin University, Changchun, Jilin 130021, P.R. China, Jilin Academy of Chinese Medicine Sciences, Jilin University, Changchun, Jilin 130021, P.R. China, School of Pharmaceutical Sciences, Jilin University, Changchun, Jilin 130021, P.R. China
  • Pages: 353-360
    |
    Published online on: December 6, 2012
       https://doi.org/10.3892/ijmm.2012.1206
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Abstract

Six novel rotundic acid (RA, 1) derivatives 4a-4f modified at the 28-COOH position were synthesized, and their structures were confirmed by IR, MS, 1H NMR and 13C NMR. The derivatives were evaluated for cytotoxic properties on the following three tumor cell lines: HeLa, HepG2 and SGC-7901. Compound 4f showed better cytotoxic activity compared with RA treatment and lower IC50 (4.16 µM) on HepG2 cells than on HeLa (8.54 µM) and SGC-7901 cells (11.32 µM). The anticancer mechanism of compound 4f was studied through cell cycle progression and apoptosis. Notably, compound 4f was able to induce apoptosis and G0/G1 cell cycle arrest of HepG2 at a concentration of 4.16 µM. In summary, RA was modified to obtain six novel derivatives. Compound 4f exhibited better cytotoxicity and may be developed as a potential agent against hepatocellular carcinoma.
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Copy and paste a formatted citation
Spandidos Publications style
Chen Y, He Y, Nan M, Sun W, Hu J, Cui A, Li F and Wang F: Novel rotundic acid derivatives: Synthesis, structural characterization and in vitro antitumor activity. Int J Mol Med 31: 353-360, 2013.
APA
Chen, Y., He, Y., Nan, M., Sun, W., Hu, J., Cui, A. ... Wang, F. (2013). Novel rotundic acid derivatives: Synthesis, structural characterization and in vitro antitumor activity. International Journal of Molecular Medicine, 31, 353-360. https://doi.org/10.3892/ijmm.2012.1206
MLA
Chen, Y., He, Y., Nan, M., Sun, W., Hu, J., Cui, A., Li, F., Wang, F."Novel rotundic acid derivatives: Synthesis, structural characterization and in vitro antitumor activity". International Journal of Molecular Medicine 31.2 (2013): 353-360.
Chicago
Chen, Y., He, Y., Nan, M., Sun, W., Hu, J., Cui, A., Li, F., Wang, F."Novel rotundic acid derivatives: Synthesis, structural characterization and in vitro antitumor activity". International Journal of Molecular Medicine 31, no. 2 (2013): 353-360. https://doi.org/10.3892/ijmm.2012.1206
Copy and paste a formatted citation
x
Spandidos Publications style
Chen Y, He Y, Nan M, Sun W, Hu J, Cui A, Li F and Wang F: Novel rotundic acid derivatives: Synthesis, structural characterization and in vitro antitumor activity. Int J Mol Med 31: 353-360, 2013.
APA
Chen, Y., He, Y., Nan, M., Sun, W., Hu, J., Cui, A. ... Wang, F. (2013). Novel rotundic acid derivatives: Synthesis, structural characterization and in vitro antitumor activity. International Journal of Molecular Medicine, 31, 353-360. https://doi.org/10.3892/ijmm.2012.1206
MLA
Chen, Y., He, Y., Nan, M., Sun, W., Hu, J., Cui, A., Li, F., Wang, F."Novel rotundic acid derivatives: Synthesis, structural characterization and in vitro antitumor activity". International Journal of Molecular Medicine 31.2 (2013): 353-360.
Chicago
Chen, Y., He, Y., Nan, M., Sun, W., Hu, J., Cui, A., Li, F., Wang, F."Novel rotundic acid derivatives: Synthesis, structural characterization and in vitro antitumor activity". International Journal of Molecular Medicine 31, no. 2 (2013): 353-360. https://doi.org/10.3892/ijmm.2012.1206
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