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Design, synthesis and pharmacological evaluation of novel 4-phenoxyquinoline derivatives as potential antitumor agents

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Chemical Research in Chinese Universities Aims and scope

Abstract

A series of novel 4-phenoxyquinoline derivatives containing 3-amino-2-cyano-acrylamide framework was designed and synthesized, and the in vitro cytotoxic activities of them against five cancer cell lines(HT-29, H460, A549, MKN-45, and U87MG) were evaluated. Most of the compounds exhibited moderate-to-significant cytotoxicity and high selectivity against one or more cell lines as compared with Foretinib. The studies of their preliminary structure-activity relationships(SARs) indicate that the compounds containing methyl groups, especially methyl groups at 4-position of the phenyl ring(moiety B) are more effective. Among them, compound 36 shows the most potent antitumor activities with IC50 values of 0.04, 0.09, 0.67, 0.39 and 1.10 μmol/L against HT-29, H460, A549, MKN-45 and U87MG cell lines, respectively.

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Authors and Affiliations

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

    Hao Hu, Mingyan Jiang, Gang Hu, Cuirong Zhang, Lixia Zhang, Shunguang Zhou, Meihui Zhang & Ping Gong

  2. Fujian Institute of Microbiology, Fuzhou, 350007, P. R. China

    Lijun Xie

Authors
  1. Hao Hu
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  2. Mingyan Jiang
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  3. Lijun Xie
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  4. Gang Hu
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  5. Cuirong Zhang
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  6. Lixia Zhang
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  7. Shunguang Zhou
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  8. Meihui Zhang
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  9. Ping Gong
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Corresponding authors

Correspondence to Meihui Zhang or Ping Gong.

Additional information

Supported by the Program for Liaoning Innovative Research Team in University, China(No.IRT1073).

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Hu, H., Jiang, M., Xie, L. et al. Design, synthesis and pharmacological evaluation of novel 4-phenoxyquinoline derivatives as potential antitumor agents. Chem. Res. Chin. Univ. 31, 746–755 (2015). https://doi.org/10.1007/s40242-015-5166-3

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  • DOI: https://doi.org/10.1007/s40242-015-5166-3

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