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Design, synthesis of amide derivatives of scutellarin and their antileukemia and neuroprotective activities

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Abstract

A unique series of amide-scutellarin derivatives were designed and synthesized in order to develop the function of scutellarin further. The antiproliferative activity of all target compounds against two human leukemia cell line was evaluated. Among them, compounds 6g and 7c displayed the most antitumor activities against HL-60 and THP-1 cells. Moreover, all compounds were also assayed for their neuroprotective activity against hydrogen peroxide (H2O2)-induced PC12 cell injury, and the majority of the compounds had moderate to good neuroprotective properties. These findings confirmed that these target compounds could be used as antileukemia or neuroprotective candidates in the future.

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Acknowledgements

We are grateful to Guiding Science and Technology Plan Project of the City of Daqing (No. zd-2020-60) and Heilongjiang Bayi Agricultural University Support Program for San Heng San Zong (No. ZRCPY201910), the central government supports local college reform and development fund talent training projects (2020GSP16), the Heilongjiang Touyan Innovation Team Program (2019HTY078) and the Project for Heilongjiang Bayi Agricultural University (XDB202012).

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Authors and Affiliations

  1. Department of Pharmaceutical Engineering, College of Life Science & Technology, Heilongjiang Bayi Agricultural University, 5 Xinfeng Road, 163319, Daqing, PR China

    Tong Han, Xing Wei, Meilin Sheng, Qin Xie, Jiqiang Zhang, Yongyi Zhang & Chenghao Jin

  2. Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, 103 Wenhua Road, 110016, Shenyang, PR China

    Chunyu Jiang

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  1. Tong Han
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Correspondence to Chenghao Jin.

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Han, T., Jiang, C., Wei, X. et al. Design, synthesis of amide derivatives of scutellarin and their antileukemia and neuroprotective activities. Med Chem Res 31, 905–915 (2022). https://doi.org/10.1007/s00044-022-02885-z

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