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Design, synthesis, and preliminary evaluation of the biological activity of dithiocarbamate-3-epi-jaspine B hybrids

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Abstract

A series of dithiocarbamate-3-epi-jaspine B hybrids have been designed and synthesized from D-xylose based on the introduction of long lipophilic alkyl dithiocarbamate moieties at the C4 position of 3-epi-jaspine B. The anticancer activities of these compounds have been evaluated against two selected tumor cell lines (MGC-803 and B16-F10 cells), with most of the synthesized compounds exhibiting moderate activity. Among them, compounds 20d and 20f showed the highest levels of inhibitory activity of all the compounds tested against MGC-803 and B16-F10 cells with IC50 values of 16.39 and 14.83 µM, respectively. This work therefore represents the first reported account of the synthesis and in vitro cytotoxic evaluation of dithiocarbamate-3-epi-jaspine B hybrids.

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Acknowledgments

The authors are grateful for the financial support from the National Natural Science Foundation of China (No. U1204206, 81172937, 81430085, 21372206).

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Authors and Affiliations

  1. School of Pharmaceutical Sciences, Institute of Drug Discovery and Development, Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, Zhengzhou University, Zhengzhou, 450001, PR China

    En Zhang, Wei-Wei Jiao, Shang Wang, Jin-Mei Xu, Xiao-Jing Shi, Yan-Chao Wang, Ya-Na Wang & Hong-Min Liu

  2. Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou, Henan Province, 450001, PR China

    En Zhang, Wei-Wei Jiao, Shang Wang, Jin-Mei Xu, Xiao-Jing Shi, Yan-Chao Wang, Ya-Na Wang & Hong-Min Liu

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  1. En Zhang
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Correspondence to Hong-Min Liu.

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Zhang, E., Jiao, WW., Wang, S. et al. Design, synthesis, and preliminary evaluation of the biological activity of dithiocarbamate-3-epi-jaspine B hybrids. Med Chem Res 25, 3011–3020 (2016). https://doi.org/10.1007/s00044-016-1721-9

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  • DOI: https://doi.org/10.1007/s00044-016-1721-9

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