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Synthesis of deuterium-enriched and fluorine-substituted plinabulin derivatives and evaluation of their antitumor activities

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Abstract

Deuterium-enriched and fluorine-substituted compounds have been widely applied in drug discovery due to their advantages in the studies of clinical pharmacokinetics and metabolic profiles. Herein we synthesized a library of deuterated and fluorine-substituted plinabulin derivatives, and all 15 D- or F-compounds were characterized by MS, \(^{1}\hbox {H}\) NMR and \(^{ 13}\hbox {C}\,\hbox {NMR}\). Their antitumor activities were evaluated against human Jurkat T lymphocyte cells.

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Acknowledgements

This work was supported by “Zhufeng Scholar Program” of Ocean University of China (841412016), “Major Projects of Independent Innovation” of Qingdao (15-4-13-zdzx-hy) and “Outstanding Talents Plan” of Qingdao (15-10-3-15-(34)-zch) to Dr. Wenbao Li.

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Authors and Affiliations

  1. Key Laboratory of Marine Drugs of Ministry of Education of China, School of Medicine and Pharmacy, Ocean University of China, Qingdao, 266003, People’s Republic of China

    Zhongpeng Ding, Tianwen Sun, Mingxu Ma, Huashi Guan & Wenbao Li

  2. Marine Biomedical Research Institute of Qingdao, Qingdao, 266071, People’s Republic of China

    Yingwei Hou, Shixiao Wang, Tianwen Sun, Huashi Guan & Wenbao Li

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  1. Zhongpeng Ding
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  2. Yingwei Hou
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  3. Shixiao Wang
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  4. Tianwen Sun
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  5. Mingxu Ma
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  6. Huashi Guan
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  7. Wenbao Li
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Correspondence to Wenbao Li.

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Ding, Z., Hou, Y., Wang, S. et al. Synthesis of deuterium-enriched and fluorine-substituted plinabulin derivatives and evaluation of their antitumor activities. Mol Divers 21, 577–583 (2017). https://doi.org/10.1007/s11030-017-9742-y

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  • DOI: https://doi.org/10.1007/s11030-017-9742-y

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