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Synthesis, in vitro and in vivo evaluation of novel substituted N-(4-(2-(4-benzylpiperazin-1-yl)ethoxy)phenyl)-N-methyl-quinazolin-4-amines as potent antitumor agents.

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机构: [1]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center of Biotherapy, Chengdu 610041, China [2]Division of Nephrology, Kidney Research Institute, West China Hospital of Sichuan University, Chengdu 610041, China
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A novel series of substituted N-(4-(2-(4-benzylpiperazin-1-yl)ethoxy)phenyl)-N-methylquinazolin-4-amines were synthesized and evaluated for their in vitro antiproliferative activity. Among them, compound 7a exhibited the best potency, with IC50 values of 0.029-0.147 μM against four types of cancer cell lines. In addition, 7a was confirmed that it could arrest the cell cycle at G2/M phase and trigger apoptosis. Indirect immunofluorescence staining revealed its anti-tubulin property. Importantly, 7a significantly inhibited tumor growths in HepG2 xenograft models without causing significant loss of body weight, suggesting that 7a is a promising new anticancer agent to be developed. Copyright © 2016 Elsevier Ltd. All rights reserved.

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出版当年[2016]版:
大类 | 3 区 医学
小类 | 3 区 药物化学 3 区 有机化学
最新[2023]版:
大类 | 4 区 医学
小类 | 2 区 有机化学 4 区 药物化学
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第一作者机构: [1]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center of Biotherapy, Chengdu 610041, China
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