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师资队伍
陈世武
职务/职称:副院长/教授/博导
研 究 所:药物化学研究所
联系电话:0931-8915587
电子邮件:chenshw@lzu.edu.cn
办 公 室:勤博楼3027室
  • 个人简介
  • 研究成果
  • 研究项目
  • 【基本情况】1994年6月毕业于西北师范大学获理学学士学位,2006年6月毕业于兰州大学获理学博士学位, 2006年11月至2008年8月在香港大学化学系作博士后研究。国家自然科学基金项目、教育部学位论文通讯评议专家,国家食药总局中保委化妆品审评专家。在科学研究方面主要从事基于结构优化的抗肿瘤药物的合成及活性研究及药物合成工艺开发等。主持和完成国家自然科学基金项目4项、甘肃省自然科学基金项目1项、中央高校基本科研业务费和校企合作项目8项。研究成果获国家科技进步二等奖一项、甘肃省科技进步二等奖一项、甘肃医学科技一等奖一项、国家发明专利三项和美国专利一项,在Eur. J. Med. Chem.、Bioorg. Chem.、Bioorg. Med. Chem.、Bioorg. Med. Chem. Lett.等国际药物化学主流期刊发表SCI论文30余篇。

    【研究方向】基于新靶点药物的设计、合成及作用机制研究,活性天然分子的结构优化及生物活性研究,药物及其中间体的合成工艺研究。

    【主讲课程】 本科生:分析化学(2014年获甘肃省精品课程称号)、药物合成反应;硕士生:药物研发概论。

    获奖情况】“藏药现代化与独一味新药创制、资源保护及产业化示范”获国家科技进步奖二等(2015-J-234-2-04,10/10),“基于拼合原理的新型鬼臼毒素类抗癌药物的发现及作用机制研究”获甘肃省科技进步奖二等(2019-J2-030,1/10),“脱氧鬼臼毒素类抗癌药物的发现及作用机制研究”获甘肃医学科技奖一等(2018-1-5,1/6),“基于桃儿七提取物鬼臼毒素的药物研究”获甘肃药学发展奖二等(2013-Y2-06,1/5)。

     

  • [1]Xing-Rong Wang, Shuai Wang, Wen-Bo Li, Kai-Yan Xu, Xue-Peng Qiao, Xue-Li Jing, Zi-Xiao Wang, Chang-jiang Yang, Shi-Wu Chen*. Design, synthesis and biological evaluation of novel 2-(4-(1H-indazol-6-yl)-1H-pyrazol-1-yl)acetamide derivatives as potent VEGFR-2 inhibitors, Eur. J. Med. Chem. 2021, 213, 113192.

    [2]Shu-Yi Hao1, Zhi-Yuan Qi1, Shuai Wang, Xing-Rong Wang, Shi-Wu Chen*. Synthesis and bioevaluation of N-(3,4,5-trimethoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-amines as tubulin polymerization inhibitors with anti-angiogenic effects. Bioorg. Med. Chem. 2021, 29, 115985.

    [3]Wen-Bo Li, Xue-Peng Qiao, Zi-Xiao Wang, Shuai Wang, Shi-Wu Chen*. Synthesis and antioxidant activity of conjugates of hydroxytyrosol and coumarin. Bioorg. Chem. 2020, 105, 104427.

    [4]Xiu-Juan Zhang, Yu Xu, Hong-Xia Mou, Shuai Wang, Shu-Yi Hao, Shi-Wu Chen*. The synthesis and anti‐tumour properties of novel 4-substituted phthalazinones as Aurora B kinase inhibitors. Bioorg. Med. Chem. Lett. 2020, 30, 127556.

    [5]Yu Xu1, Xiu-Juan Zhang1, Wen-Bo Li, Xing-Rong Wang, Xue-Peng Qiao, Shi-Wu Chen*. Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors. Eur. J. Med. Chem. 2020, 208, 112780.

    [6]Zhi-Yuan Qi, Shu-Yi Hao, Heng-Zhi Tian, Hong-Li Bian, Ling Hui, Shi-Wu Chen*. Synthesis and biological evaluation of 1-(benzofuran-3-yl)-4-(3,4,5-trimethoxyphenyl)-1H-1,2,3-triazole derivatives as tubulin polymerization inhibitors. Bioorg. Chem. 2020, 94, 103392.

    [7]Yong-Xin Bo, Rong Xiang, Yu Xu, Shu-Yi Hao, Xing-Rong Wang, Shi-Wu Chen*. Synthesis, biological evaluation and molecular modeling study of 2-amino-3,5-disubstituted-pyrazines as Aurora kinases inhibitors. Bioorg. Med. Chem. 2020, 28 (5), 115351.

    [8]Yu Xu, Shu-Yi Hao, Xiu-Juan Zhang, Wen-Bo Li, Xue-Peng Qiao, Zi-Xiao Wang, Shi-Wu Chen*. Development of novel 2,4-disubstituted pyrimidine derivatives as Aurora kinase inhibitors. Bioorg. Med. Chem. Lett. 2020, 30 (3), 126885.

    [9]Shu-Yi Hao, Shi-Liang Feng, Xing-Rong Wang, Zhichao Wang, Shi-Wu Chen*, Ling Hui**. Novel conjugates of podophyllotoxin and coumarin: Synthesis, Cytotoxities, Cell cycle arrest and Inhibition of TOPO-Ⅱβ. Bioorg. Med. Chem. Lett. 2019, 29 (16), 2129–2135.

    [10]You-Zhen Ma, Zhen-Bo Tang, Chun-Yan Sang, Zhi-Yuan Qi, Ling Hui, Shi-Wu Chen*. Synthesis and biological evaluation of nitroxide labeled pyrimidines as Aurora kinase inhibitors. Bioorg. Med. Chem. Lett. 2019, 29 (5), 694–699.

    [11]Chun-Yan Sang, Wen-Wen Qin, Xiu-Juan Zhang, Yu Xu, You-Zhen Ma, Xing-Rong Wang, Ling Hui, Shi-Wu Chen*. Synthesis and identification of 2,4-bisanilinopyrimidines bearing 2,2,6,6-tetramethylpiperidine-N-oxyl as potential Aurora A inhibitors. Bioorg. Med. Chem. 2019, 27 (1), 65–78.

    [12]You-Zhen Ma, Zhen-Bo Tang, Chun-Yan Sang, Zhi-Yuan Qi, Ling Hui, Shi-Wu Chen*. Synthesis and biological evaluation of nitroxide labeled pyrimidines as Aurora kinase inhibitors. Bioorg. Med. Chem. Lett. 2019, 29 (5), 694–699.

    [13]Wei Wang, Xiu Feng, Huan-Xiang Liu, Shi-Wu Chen*, Ling Hui. Synthesis and biological evaluation of 2,4-disubstituted phthalazinones as Aurora kinase inhibitors. Bioorg. Med. Chem. 2018, 26 (13), 3217–3226.

    [14]Chun-Yan Sang, Heng-Zhi Tian, Yue Chen, Jian-Fei Liu, Shi-Wu Chen*, Ling Hui.  Synthesis and biological evaluation of 4β-(thiazol-2-yl)amino-4′-O-demethyl-4-deoxypodophyllotoxins as topoisomerase-II inhibitors. Bioorg. Med. Chem. Lett. 2018, 28 (2), 71–76.

    [15]Xiao-Hui Xu, Xiao-Wen Guan, Shi-Liang Feng, You-Zhen Ma, Shi-Wu Chen*, Ling Hui*. One-pot synthesis and biological evaluation of N-(aminosulfonyl)-4-podophyllotoxin carbamates as potential anticancer agents. Bioorg. Med. Chem. Lett. 2017, 27(13), 2890–2894.

    [16]Zhen-Bo Tang, Yao-Zhang Chen, Jie Zhao, Xiao-Wen Guan, Yong-Xin Bo, Shi-Wu Chen*, Ling Hui* Conjugates of podophyllotoxin and norcantharidin as dual inhibitors of topoisomeraseⅡ and protein phosphatase 2A. Eur. J. Med. Chem. 2016, 123, 568–576.

    [17]Xiao-Wen Guan, Xiao-Hui Xu, Shi-Liang Feng, Zhen-Bo Tang, Shi-Wu Chen*, Ling Hui Synthesis of hybrid 4-deoxypodophyllotoxin–5-fluorouracil compounds that inhibit cellular migration and induce cell cycle arrest. Bioorg. Med. Chem. Lett. 2016, 26(6), 1561–1566.

    [18]Ling Hui*, Chun-Yan Sang, Dong-Hong Wang, Xiao-Hui Wang, Mei-Liang Wang, Qing-Hua Jia, Ming-Ren Ma, Shi-Wu Chen* Newly synthesized podophyllotoxin derivative, LJ12, induces apoptosis and mitotic catastrophe in non-small cell lung cancer cells in vitro. Molecular Medicine Reports, 2016. 13: 339–346.

    [19]Wen-Wen Qin, Chun-Yan Sang, Lin-Lin Zhang, Wei Wei, Heng-Zhi Tian, Huan-Xiang Liu, Shi-Wu Chen*, Ling Hui* Synthesis and biological evaluation of 2,4-diaminepyrimides as selective Aurora A kinase inhibitors. Eur. J. Med. Chem. 2015, 95, 174–184.

          [20]Jie Zhao, Xiao-Wen Guan, Shi-Wu Chen*, Ling Hui Synthesis and biological evaluation of norcantharidin derivatives as protein phosphatase-1 inhibitors. Bioorg. Med. Chem. Lett. 2015, 25(2), 363–366. 

        发明专利: 

       1.陈世武,田瑄和涂永强,鬼臼脂素类化合物及其应用与制备方法,中国发明专利:ZL2004 1 0026068.3.

       2.Dan Yang, Cheng-Yong Li and Shi-Wu Chen. 5-Demethoxyfumagillol and derivatives thereof. US Patent, US899067 B2.

       3.陈世武,惠玲和金岩,一种脱氧鬼臼毒素类化合物及其制备与应用,中国发明专利:201110004251.3.

       4.陈世武,向蓉和惠玲,一种脱氧鬼臼与5-氟尿嘧啶的拼合物及其制备与应用,中国发明专利:201110125795.5.

       5.陈世武,赵杰和惠玲,一种鬼臼毒素与去甲斑蝥素的拼合物及其制备与应用,中国发明专利, ZL201510740485.2(公告号CN106632405B)

       6.陈世武,孛永鑫,一种3,5-二取代的二氨基吡嗪化合物及其制备工艺与应用,中国发明专利:ZL201810212197.3(公告号CN106632405B)

       7.陈世武,王维 一种肽嗪酮化合物及其制备与应用 中国发明专利 ZL201810212221.3(申请日期:2018.03.15)(2020.12.29授权)(公告号CN108250150A)


     

  •         [1]稳定氮氧自由基标记的极光激酶A抑制剂的合成及生物活性研究(21372110),国家自然科学基金面上项目,20142017,项目负责人。

    [2]自旋标记Aurora-A激酶抑制剂的合成及生物活性研究(1208RJZA247),甘肃省自然科学基金项目,20122014,项目负责人。

    [3]泰拉霉素原料药及相关物质的结构研究,山东鲁抗舍里乐药业有限公司,校企合作项目,20152016,项目负责人。

    [4]基于骨架迁越的肽嗪类极光激酶A和VEGFR-2双靶点抑制剂的合成及生物活性的研究(21672093),国家自然科学基金面上项目, 20172020,项目负责人。

    [5]泰地罗新原料药的制备工艺,山东鲁抗舍里乐药业有限公司,校企合作项目,20172018,项目负责人。

    [6]非罗考昔原料药的制备工艺,山东鲁抗舍里乐药业有限公司,校企合作项目,20182020,项目负责人。

            [7]氟雷拉纳原料药的制备工艺,山东鲁抗舍里乐药业有限公司,校企合作项目,20192021,项目负责人。



     

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