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Synthesis and biological activity of imidazo[4,5-c]quinoline derivatives as PI3K/mTOR inhibitors

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Abstract

A series of imidazo[4,5-c]quinoline derivatives(12a—12m) was synthesized with 2-amino-5-bromobenzoic acid and 4-nitrophenylacetonitrile as starting materials, 6-bromo-4-chloro-3-nitroquinoline as intermediate and Suzuki reaction and closure of the imidazolinone ring with triphosgene as key steps. The structures of the key intermediate and target compounds were confirmed by means of 1H NMR, 13C NMR and HRMS. These compounds show an interesting kinase profile as dual PI3K/mTOR tool compounds.

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Authors and Affiliations

  1. College of Pharmacy, Jilin University, Changchun, 130012, P. R. China

    Yanjie Li, Shengxiu Niu, Yanping Zhao, Lijuan Yang, Xiaowei Shao & Ensi Wang

  2. College of Pharmacy, Changchun University of Traditional Chinese Medicine, Changchun, 130117, P. R. China

    Yanjie Li

  3. Beijing Foreland Pharma Biological Technology Co., Ltd, Beijing, 101111, P. R. China

    Xingmin Zhang

Authors
  1. Yanjie Li
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  2. Xingmin Zhang
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  3. Shengxiu Niu
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  4. Yanping Zhao
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  5. Lijuan Yang
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  6. Xiaowei Shao
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  7. Ensi Wang
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Corresponding author

Correspondence to Ensi Wang.

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Supported by the Fund of Jilin University(China) Hi-Tech(Group) Co., Ltd.

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Li, Y., Zhang, X., Niu, S. et al. Synthesis and biological activity of imidazo[4,5-c]quinoline derivatives as PI3K/mTOR inhibitors. Chem. Res. Chin. Univ. 33, 895–902 (2017). https://doi.org/10.1007/s40242-017-7074-1

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  • DOI: https://doi.org/10.1007/s40242-017-7074-1

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