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Synthesis and bioactivity of novel coumarin derivatives

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Chemistry of Heterocyclic Compounds Aims and scope

A series of novel coumarin derivatives were synthesized from commercially available chemical agents. All prepared compounds were evaluated for their in vitro antiproliferative activity against five selected human cancer cell lines (EC109, MGC-803, PC-3, MCF-7, and EC9706) and their in vitro antimicrobial activity against E. coli and M. albicans. 4-(3-Bromopropoxy)-2H-chromen-2-one exhibited the highest growth inhibition against MGC-803 cell line (IC50 47.7 μM) and 7-(2-bromoethoxy)-2H-chromen-2-one exhibited the highest growth inhibition against MCF-7 cell line (IC50 48.3 μM). The latter compound was also the most active against E. coli (MIC50 0.27 μg/ml).

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The authors are grateful for the financial support from the National Natural Science Foundation of China (No. 81273393).

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Authors and Affiliations

  1. Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, 450001, PR China

    Sai-Yang Zhang, Dong-Jun Fu, Hui-Hui Sun, Ying-Chao Liu, Yan-Bing Zhang & Hong-Min Liu

  2. Henan Medical College, Zhengzhou, 450001, PR China

    Xiao-Xin Yue

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  1. Sai-Yang Zhang
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  2. Dong-Jun Fu
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  3. Hui-Hui Sun
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  4. Xiao-Xin Yue
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  5. Ying-Chao Liu
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  6. Yan-Bing Zhang
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  7. Hong-Min Liu
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Correspondence to Yan-Bing Zhang.

Additional information

Supplementary information file to this article containing the 1H and 13C NMR spectra of the synthesized compounds is available at http://link.springer.com/journal/10593.

Published in Khimiya Geterotsiklicheskikh Soedinenii, 2016, 52(6), 374–378

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Zhang, SY., Fu, DJ., Sun, HH. et al. Synthesis and bioactivity of novel coumarin derivatives. Chem Heterocycl Comp 52, 374–378 (2016). https://doi.org/10.1007/s10593-016-1898-3

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  • DOI: https://doi.org/10.1007/s10593-016-1898-3

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