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Design, synthesis and antitumor activity of pyrrolopyrazinone-chalcone hybrids

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Abstract

A series of pyrrolopyrazinone-chalcone hybrids(12a–12q) was designed, synthesized and screened for their antitumor activity against SKOV-3, A549 and HeLa cell lines in vitro. Compared with the pyrrolopyrazinone( 10a) and 5-fluorouracil(5-FU), nearly all the tested compounds showed significantly-improved antitumor activities. The most promising compounds 12e and 12k(IC50=0.25 and 0.88 μmol/L) respectively show activities of 123 and 35 times that of compound 10a(IC50=30.74 μmol/L) against HeLa cell line. The result reveals that the presence of chalcone moiety is beneficial to their activity and selectivity.

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Authors and Affiliations

  1. Key Laboratory of Structure-based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, P. R. China

    Ying Meng, Hongwei Zhang, Zehua Liu, Shanchao Zeng, Hongwei Zhang, Chiyu Sun, Lijuan Zhang, Mingming Zhao & Hongrui Song

  2. Key Laboratory for Molecular Enzymology & Engineering, Ministry of Education, Jilin University, Changchun, 130012, P. R. China

    Guan Wang, Mengying Jiang & Wei Shi

Authors
  1. Ying Meng
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  2. Hongwei Zhang
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  3. Zehua Liu
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  4. Shanchao Zeng
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  5. Hongwei Zhang
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  6. Chiyu Sun
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  7. Lijuan Zhang
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  9. Guan Wang
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  10. Mengying Jiang
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  11. Wei Shi
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  12. Hongrui Song
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Corresponding author

Correspondence to Hongrui Song.

Additional information

Supported by the Program for Liaoning Innovative Research Team in University, China(No.2007T177).

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Meng, Y., Zhang, H., Liu, Z. et al. Design, synthesis and antitumor activity of pyrrolopyrazinone-chalcone hybrids. Chem. Res. Chin. Univ. 30, 624–631 (2014). https://doi.org/10.1007/s40242-014-3542-z

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  • DOI: https://doi.org/10.1007/s40242-014-3542-z

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