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药物化学博士生导师--徐云根

  徐云根,教授,博士生导师,江苏省第六届十大杰出专利发明人,江苏省高校“青蓝工程”中青年学术带头人。现任药学院药物化学系主任,江苏省药物分子设计与成药性优化重点实验室副主任,江苏省高校优秀科技创新团队负责人,中国药科大学校学术委员会委员。兼任中国药学会药物化学专业委员会副主任委员,江苏省药学会药物化学专业委员会副主任委员,国家执业药师资格考试命审题专家,国家重点研发计划等评审专家,《中国现代应用药学》等杂志编委;担任 Organic Chemistry, Current Medicinal Chemistry, Biochemical Pharmacology, European Journal of Medicinal Chemistry, Bioorganic & Medicinal Chemistry, Carbohydrate Research等国际杂志特约审稿人。
       主要从事新药分子的设计与合成、药物合成新技术与新工艺等方向的研究工作。近年来,专注于镇痛、抗炎、抗肿瘤和心脑血管药物的研究,在活性天然产物的结构改造和成药性优化、个体化抗肿瘤药物的设计与合成、药物合成新技术和新工艺等方面开展了卓有成效的研究,取得了一些阶段性成果,目前有两个候选药物已进入临床前评价。
       近年来,作为课题负责人,先后主持国家重大新药创制科技重大专项(2项)、国家自然科学基金(4项)、省部级科技计划(10余项)和横向开发项目(5项)的研究工作。申请发明专利70余个,已获得授权专利48个,包括美国、加拿大等外国专利6个;有多个专利产品或技术已实施转让或产业化,取得了良好的经济效益。在国内外核心刊物上发表论文100余篇,其中在Organic Letters, Green Chemistry, European Journal of Medicinal Chemistry, Organic & Biomolecular Chemistry, Carbohydrate Research等期刊发表SCI论文60余篇。
       联系方式:025-83271244;  Email:xyg64@126.com;xyg@cpu.edu.cn

       近三年发表的部分论文:
   1. Qihua Zhu, Dezhong Ji, Tingting Liang, Xueyan Wang, Yungen Xu*. Efficient Palladium-Catalyzed C−H Fluorination of C(sp3)−H Bonds: Synthesis of βFluorinated Carboxylic Acids. Org Lett, 17, 3798−3801, 2015.
      2. Zong-jie Gan, Yu-hua Wang, Yungen Xu*, Ting Guo, Jun Wang, Qiao Song, Xue-jun Xu, Shi-yuan Hu, Yu-jun Wang, De-chuan Wang, De-zhu Sun, Di Zhang, Tao Xi, Hao-dong Li, Hai-bo Zhang, Taijun Hang, Hong-guo Lu, Jing-gen Liu*. Discovery, Stereospecific Characterization and Peripheral Modification of 1-(Pyrrolidin-1-ylmethyl)-2-[(6-chloro-3- oxo-indan)-formyl]- 1,2,3,4-tetrahydroisoquinolines As Novel Selective k Opioid Receptor Agonists. Org Biomol Chem, 20(13), 5656-5673, 2015.
      3. Shaochi Wang, Peng Dai, Yungen Xu*, Qiufang Chen, Qihua Zhu, Guoqing Gong*. Design, Synthesis, and Biological Evaluation of Dabigatran Etexilate Mimics, a Novel Class of Thrombin Inhibitors. Arch Pharm Chem. Life Sci, 348, 595–605, 2015.
      4. Chen Zhou, Fangxia Zou, Yungen Xu*, Luyong Zhang, Xiaoming Zha*, Identification of New Non-steroidal TGR5 Agonists Using Virtual Screening with Combined Pharmacophore Models. Med Chem Res, 24(6):2561-2572,2015.
      5. Chen Zhou, Di Kang, Yungen Xu*, Luyong Zhang, Xiaoming Zha*, Identification of Novel Selective LSD1 Inhibitors Using a Pharmacophore Based Virtual Screening Combined with Multiple Docking. Chem Biol Drug Design, 6:659-671, 2015.
      6. Dong-Xing Chen, Jie Huang, Meng Liu, Yun-Gen Xu*, Cheng Jiang*. Design, Synthesis, and Evaluation of Non-ATP-Competitive Small-Molecule Polo-Like Kinase 1 (Plk1) Inhibitors. Arch Pharm Chem. Life Sci, 348(1):2–9, 2015.
     7. Qiao Song,Dongmei Zhang, Qihua Zhu*, Yungen Xu*. p-Toluenesulfonohydrazide as Highly Efficient Initiator for Direct C−H Arylation of Unactivated Arenes. Org Lett, 16(20): 5272-5274, 2014.
     8. Xiaobo Bao, Wei Yao, Qihua Zhu*, Yungen Xu*. Synthesis of 6-substituted phenanthridine derivatives by Palladium-Catalyzed Domino Suzuki-Miyaura/ Aza-Michael Reactions. Eur J Org Chem, (33):7443-7450, 2014.
     9. Lei Shi*, Ting-Ting Wu, Zhi Wang, Jia-Yu Xue, Yun-Gen Xu*. Discovery of N-(2-phenyl-1H-benzo[d]imidazol-5-yl)quinolin-4-amine derivatives as novel VEGFR-2 kinase inhibitors. Eur J Med Chem, 84:698-707, 2014.
      10. Yun Yang, Xinhui Wang, Qihua Zhu, Guoqing Gong*, Danmeng Luo, Aidou Jiang, Liyan Yang, Yungen Xu*. Synthesis and pharmacological evaluation of novel limonin derivatives as anti-inflammatory and analgesic agents with high water solubility. Bioorg Med Chem Lett, 24(7):1851-1855, 2014.
      11. Jinyin Li, Jing Fang, Fanyi Zhong, Wenxue Li, Yuanjun Tang, Yungen Xu, Shilong Mao*, Guorong Fan*. Development and validation of a liquid chromatography/tandem mass spectrometry assay for the simultaneous determination of dabigatran etexilate, intermediate metabolite and dabigatran in 50 μL rat plasma and its application to pharmacokinetic study. Journal of Chromatography B. 973, 110–119, 2014.
      12. Kun Liu, Shuowei Yao,Yinghan Lou, Yungen Xu*. Synthesis and anti-angiogenetic activity evaluation of N-(3-aryl acryloyl)aminosaccharide derivatives. Carbohyd Res, 381:83-92,2013.
      13. Yan Tang, Zhewei Tu, Jing Sun, Xiong Zhu*, Kun Liu, Shuying He, Yungen Xu*. Design, Synthesis and Biological Evaluation of Novel Aminosaccharide Derivatives of Combretastatin A-4. Lett Drug Des Discov,10(10): 935-941,2013.
      14. QihuaZhu, XuyangWang, Zhaoxing Chu, Guangwei He*, Guangping Dong, YungenXu*. Design, synthesis and biological evaluation of novel imidazo[4,5-c]pyridinecarboxamide derivatives as PARP-1 inhibitors. Bioorg Med Chem Lett, 23(7):1993-6,2013.
      15. Yun-Zhan Li, Guo-Qing Gong*, Wen-Hui Yang, Xin-Hui Wang, Mei-Ling Jiang, Yi Zhou, Xiao-Zhi Yang, Yun-Gen Xu*, Guang-Wei He. Antithrombotic activity of HY023016, a novel Dabigatran prodrug evaluated in animal thrombosis models. Thrombosis Research, 131(5), 425-435,2013.
      16. Haiping Zhou, Huiting Su, Zongjie Gan, Dechuan Wang, Yungen Xu*. An efficient procedure for synthesis of 2, 3-dihydro-1Hindene-1-methanamines. Res Chem Intermed, 39:4091-4098, 2013.
      17. Zhi Wang, Yi-Qiao Fan, Lei Shi*, Yun-Gen Xu*. Synthesis, crystal structure, and biological activities of a Zn(II) complex with a Se substituted Schiff base. J Coord Chem, 66(11): 2032-2038, 2013.
      18. Xiao-Zhi Yang, Xiao-Juan Diao, Wen-Hui Yang, Feng Li, Guang-Wei He, Guo-Qing Gong, Yun-Gen Xu*. Design, synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing methyl ferulate. Bioorg Med Chem Lett, 23: 2089-2092,2013.
      19. Xu Zhang, Ting Peng, Xun Ji, Jian Li, Linjiang Tong, Zeng Li, Wei Yang, Yungen Xu, Mengyuan Li, Jian Ding, Hualiang Jiang, Hua Xie, Hong Liu*. Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor. Bioorg Med Chem, 21(24):7988-7998, 2013.
      20. Bin Hu, Qiao Song, Yungen Xu*. Scale-up Synthesis of Antidepressant Drug Vilazodone. Org Process Res Dev, 16(9):1552-1557,2012.
      21. Xiao-Zhi Yang, Wen-Hui Yang, Yun-Gen Xu*, Xiao-Juan Diao, Guang-Wei He, Guo-Qing Gong*. Synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing a cleavable moiety with anti-platelet activity. Eur J Med Chem, 57: 21-28, 2012.
      22. Yi Zhou, Guoqing Gong*, Wenhui Yang , Yin Wang, Jing Xu, Yungen Xu. The cardioprotective effect of TG-6, a newly synthesized compound, on ischemia-reperfusion injury in rats. Eur J Pharmacol, 683(1-3):190-196,2012.
      23. 靳璐, 姜向敏, 何广卫*, 徐文婷, 龚国清, 徐云根*. 4(6)-{2-[4-(2,3,4-三甲氧基苄基)哌嗪-1-基]-2-氧代乙氧基}芳甲酰胍类化合物的合成及其Na+/H+交换器-1抑制活性, 有机化学. 32(2): 326-332,2012.
      24. Jin Ning, Yang Yun, Xu Wenting, Yang Xiaozhi, Gong Guoqing, Xu Yungen*. Synthesis and Bioactivity of Substituted Benzoylguanidine Derivatives as Potent Na+/H+ Exchanger Inhibitors. Chin J Chem, 30(2):333-340,2012.
      25. Zongjie Gan, Bin Hu, Qiao Song, Yungen Xu*. Convenient Chlorination of Some Special Aromatic Compounds using N-Chlorosuccinimide. Synthesis-Stuttgart, 44(7):1074-1078,2012.
      26. Qihua Zhu, Xuyan Wang, Yungen Xu*. Palladium-Catalyzed Tandem Reactions of β-(2-Bromophenyl)-α,β-Unsaturated Carbonyl Compounds with 2-Hydroxyphenylboronic Acid: A New Route to Benzo[c]chromenes. Eur J Org Chem, 6: 1112-1114, 2012.
      出版的主要论著或教材:
      1.《Medicinal Chemistry》(Second Edition),科学出版社,2012年9月第二版,编者。
      2.《药物化学》,中国医药科技出版社,2011年2月第二版,副主编。
      3.国家执业药师资格考试应试指南《药学专业知识》(二),中国医药科技出版社,2011年1月第一版,编者。
      4.《药物化学》,人民卫生出版社,2011年8月第七版,编者。
      5.《药物化学实验方法学》,人民卫生出版社,2010年6月出版,编者。
      6.《药物化学》,化学工业出版社,2015年8月出版,编者。
      7.《药物化学实验与指导》(双语),中国医药科技出版社,2008年8月出版,副主编。
      8.《药物设计学》,人民卫生出版社,2007年8月第一版,编者。


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