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Design, synthesis and antitumor activity of aromatic urea-quinazolines

    Zhao Yang

    Department of Medicinal Chemistry, School of Pharmacy, Hebei Medical University, Hebei, Shijiazhuang 050017, PR China

    ‡Authors contributed equally

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    ,
    Jian-Min Gu

    Department of Medicinal Chemistry, School of Pharmacy, Hebei Medical University, Hebei, Shijiazhuang 050017, PR China

    ‡Authors contributed equally

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    ,
    Qiu-Ya Ma

    Department of Medicinal Chemistry, School of Pharmacy, Hebei Medical University, Hebei, Shijiazhuang 050017, PR China

    ,
    Na Xue

    Department of Medicinal Chemistry, School of Pharmacy, Hebei Medical University, Hebei, Shijiazhuang 050017, PR China

    Department of Pharmaceutical Engineering, Hebei Chemical & Pharmaceutical College, Hebei, Shijiazhuang 050026, PR China

    ,
    Xiao-Wei Shi

    Department of Medicinal Chemistry, School of Pharmacy, Hebei Medical University, Hebei, Shijiazhuang 050017, PR China

    ,
    Lei Wang

    Department of Medicinal Chemistry, School of Pharmacy, Hebei Medical University, Hebei, Shijiazhuang 050017, PR China

    ,
    Kai Zhang

    *Author for correspondence: Tel.: +86 0311 86265624; Fax: +86 0311 86052053;

    E-mail Address: zhk810728@163.com

    Department of Medicinal Chemistry, School of Pharmacy, Hebei Medical University, Hebei, Shijiazhuang 050017, PR China

    ,
    Ya-Bo Wang

    Department of Medicinal Chemistry, School of Pharmacy, Hebei Medical University, Hebei, Shijiazhuang 050017, PR China

    ,
    De-Ying Cao

    Department of Medicinal Chemistry, School of Pharmacy, Hebei Medical University, Hebei, Shijiazhuang 050017, PR China

    ,
    Ran Guo

    Department of Medicinal Chemistry, School of Pharmacy, Hebei Medical University, Hebei, Shijiazhuang 050017, PR China

    &
    Rui-Juan Xing

    Department of Medicinal Chemistry, School of Pharmacy, Hebei Medical University, Hebei, Shijiazhuang 050017, PR China

    Published Online:https://doi.org/10.4155/fmc-2019-0220

    Background: Gefitinib and sorafenib have been proved effective for the treatment of cancers in clinical practice for years. Materials & methods: We intended to integrate the structural features of gefitinib and sorafenib and construct structurally unique 7-aromatic ureido-4-anilinoquinazolines. Results: Most of the targets exhibited promising antitumor activities. 8u showed excellent antitumor activities against the three tested cell lines (IC50, 0.81–2.49 μM). The enzymatic, apoptosis assay of 8u were also performed to study their preliminary action of mechanism. Conclusion: 8u deserve further research as antitumor agents.

    Graphical abstract

    Papers of special note have been highlighted as: • of interest; •• of considerable interest

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