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药物化学博士生导师--徐进宜

   徐进宜,药学博士,中国药科大学药学院药物化学系教授,博导。1986年毕业于中国药科大学,留校任教30年,一直工作在教学科研第一线,先后讲授了药物化学、药物合成反应、药物分子设计、药学英语、专业英语等课程。协助指导和独立指导过博士、硕士研究生50余名。在国内外期刊发表论文100余篇,其中SCI论文80余篇;申请国内外发明专利20余项,授权14项;参编著作10部。获得“教书育人”优秀教师奖;教育部优秀青年教师;国家科技部优秀论文二等奖;广东省科学技术奖励一等奖;中国药科大学先进科技工作者等荣誉。
   担任国家863计划评审专家、国家自然科学基金评审专家、农业部兽药审评、江苏省新药审评专家;担任Journal of Medicinal Chemistry, Current Medicinal ChemistryEuropean Journal of Medicinal Chemistry, Bioorganic & Medicinal Chemistry等国际杂志特约审稿人。
   研究方向:
     1. 活性天然产物的合成、结构优化及生物活性研究:基于具有生物活性天然产物的结构,研究其可能的作用机制及合成方法,发现其具有活性的最简化学结构,并针对成药性进行结构优化研究(硕士招生方向)。
     2.  针对重大疾病的创新药物研究:对严重危害人类健康的重大疾病,根据其相关的生理、生化知识,开展药物分子的创新设计、合成和成药性优化研究(博士招生方向)。
       研究经历:
       
天然活性产物23-羟基白桦酸的结构改造、生物活性与构效关系研究;喜树碱类分子结构修饰与生物活性研究;天然活性产物XJP全合成及其类似物的新药设计研究;冬凌草甲素的结构改造与生物活性研究;四环二萜类活性天然产物化合物库的构建、生物学评价及作用机制研究;非肽类血管紧张素II受体拮抗剂的设计与合成研究;AT1受体拮抗剂类新药氯沙坦、依贝沙坦、坎地沙坦的合成工艺研究;血管紧张素AT1受体和内皮素ETA受体双重拮抗剂研究;新型抗高血压药物及抗心衰药物ATPT的研究;非苯二氮卓类GABAA受体激动剂的研究;COX-2/5-LOX双重抑制剂的研究;手性Ocotillol型人参皂苷结构修饰衍生物的设计与合成研究;β-榄香烯结构修饰衍生物的设计合成与构效关系研究;在日本近畿大学完成了天然活性产物Gregatin B的全合成及结构修饰研究。
       科研项目:
       
负责承担了十一五“重大新药创制”、国家自然科学基金、国家科技支撑计划、教育部科学技术研究重点项目、高等学校博士学科点专项科研基金、长三角科技攻关、江苏省自然科学基金、江苏省医药科技攻关等国家和省部级项目的研究。
        近期代表性SCI论文

  1.Jie Liu, HaoRen, Jinyi Xu*, RenrenBai, Qi Yan, Wenlong Huang, Xiaoming Wu*, Jihua Fu, Qiujuan Wang, Qian Wu, Rong Fu. Total synthesis and antihypertensive activity of 7,8-dihydroxy-3-methyl-isochromanone-4. Bioorg.& Med. Chem. Lett., 2009, 19: 1822-1824.(IF 2.661)
  2.Lei Wang,Dahong Li, Yihua Zhang*, Jinyi Xu*. Recent progress in the development of natural ent-kauranediterpenoids with anti-tumor activity. Mini-Rev. Med. Chem. 2011, 11, 910-919. (IF 2.528)
  3.Chao Lei Wang, Bing-Feng Sun*, Shu-Guang Chen, Rui Ding, Guo-Qiang Lin*, Jinyi Xu*, Yong-Jia Shang.Concise Formal Synthesis of (+)-Englerin A and Total Synthesis of (–)-Orientalol F: Establishment of the Stereochemistry of the Organocatalytic [4+3]-Cycloaddition Reaction. Synlett, 2012, 23, 263–266. (IF 2.710)
  4.Fei Sun, Peiqing Zhu, Hequan Yao, Xiaoming Wu*, Jinyi Xu*. A partial synthesis of 23-hydroxybetulonic acid and 23-hydroxybetulinic acid starting from betulinic acid. J. Chem. Res., 2012, 36(5): 254-257. (IF 0.921)
  5.Renren Bai, Xue Yang, Yao Zhu, Zhiwen Zhou, WeijiaXie, Hequan Yao, Jieyun Jiang, Jie Liu*, MingqinShen, Xiaoming Wu, Jinyi Xu*. Novel nitric oxide-releasing isochroman-4-one derivatives: Synthesis and evaluation of antihypertensive activity. Bioorg.& Med. Chem., 2012, 20 (23): 6848-6855. (IF 2.921)
  6.Renren Bai, Zhen Wei, Jie Liu, WeijiaXie, Hequan Yao, Xiaoming Wu*, Jieyun Jiang, Qiujuan Wang and Jinyi Xu*. Synthesis and biological evaluation of 4′-[(benzimidazole-1-yl)methyl] biphenyl-2-sulfonamide derivatives as dual angiotensin II/endothelin A receptor antagonists. Bioorg.& Med. Chem., 2012, 20 (15): 4661-4667. (IF 2.921)
  7.Renren Bai, Jie Liu, Yao Zhu, Xue Yang, Chen Yang, Lingyi Kong, Xiaobing Wang, Hengyuan Zhang, Hequan Yao, MingqinShen, Xiaoming Wu*, Jinyi Xu*.Chiral separation, configurational identification and antihypertensive evaluation of (±)-7,8-dihydroxy-3-methyl-isochromanone-4. Bioorg.& Med. Chem. Lett., 2012, 22 (20), 6490-6493. (IF2.661)
  8.Lei Wang, Dahong Li, ShengtaoXu, Hequan Yao, Yihua Zhang*, Jieyun Jiang, Jinyi Xu* .The conversion of oridonin to spirolactone-type or enmein-type diterpenoid: synthesis and biological evaluation of ent-6,7-seco-oridonin derivatives as novel potential anticancer agents. Eur. J. Med. Chem.2012, 52, 242-250. (IF3.499)   
  9.Xiaoli Wang, Qian Zhao, Xuliang Wang, Tingting Li, Yisheng Lai, SixunPeng, HuiJi, Jinyi Xu*, Yihua Zhang*.Studies on the enantiomers of ZJM-289: synthesis and biological evaluation of antiplatelet, antithrombotic and neuroprotective activities. Organic &Biomolecular Chemistry, 2012, 10(45): 9030-9040. (IF 3.696)
  10.Dahong Li, HaoCai, Bowen Jiang, Guyue Liu, Yuetong Wang, Lei Wang, Hequan Yao, Xiaoming Wu*, Yijun Sun, Jinyi Xu*. Synthesis of spirolactone-type diterpenoid derivatives from kaurene-type oridonin with improved antiproliferative effects and their apoptosis-inducing activity in human hepatoma Bel-7402 cells.Eur. J. Med. Chem.2013, 59, 322-328. (IF3.499)
  11.RenrenBai, Xue Yang, Wen Hong, Yiqun Tang, Hequan Yao, Jieyun Jiang, Jie Liu, MingqinShen, Xiaoming Wu*, Jinyi Xu*.Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. Bioorg.& Med. Chem., 2013, 21: 2495-2502. (IF 2.921)
  12.ShengtaoXu, Yu Zhou, Jinyi Xu*, Hualiang Jiang,Hong Liu*. Gold-catalyzed Michael Addition/Intramolecular Annulation Cascade: an Effective Pathway for the Chemoselective and Regioselective Synthesis of Tetracyclic Indole Derivatives in Water. Green Chem., 2013, 15, 718-726. (IF 6.320)
  13.Xiaoli Wang, Linna Wang, Tingting Li, Zhangjian Huang, Yisheng Lai, HuiJi, Xiaolong Wan, Jinyi Xu*, Yihua Zhang*. Novel Hybrids of Optically Active Ring-Opening 3-n-Butylphthalide Derivative and Isosorbide as Potential Anti-Ischemic Stroke Agents. J Med. Chem., 2013, 56, 3078-3089. (IF 5.614)
  14.Dahong Li, ShengtaoXu, HaoCai, Lingling Pei, Lei Wang, Hequan Yao, Xiaoming Wu*, Jieyun Jiang, Yijun Sun, Jinyi Xu*.Library construction and biological evaluation of novel enmein-type diterpenoid analogs as potential anticancer agents. Chem .Med. Chem., 2013, 8: 812-818.(IF 3.151)
  15.Dahong Li, ShengtaoXu, HaoCai, Lingling Pei, Hengyuan Zhang, Lei Wang, Hequan Yao, Xiaoming Wu*, Jieyun Jiang, Yijun Sun, Jinyi Xu*. Enmein-type diterpenoid analogs from natural kaurene-type oridonin: synthesis and their antitumor biological evaluation Eur. J. Med. Chem. 2013, 64, 215-221. (IF 3.499)
  16.Ziwen Zhou, Cong Ma, Hengyuan Zhang, Y Bi, Xia Chen, HuaTian, XiaoniXie, QingguoMeng, Peter John Lewis*, Jinyi Xu*. Synthesis and Biological Evaluation of Novel Ocotillol-Type Triterpenoid Derivatives as Antibacterial Agents. Eur. J. Med. Chem2013, 68, 444-453. (IF 3.499)
  17.Bo Jiang, Xiaojing Huang, Hequan Yao, Jieyun Jiang, Xiaoming Wu*, Siyi Jiang, Qiujuan Wang, Tao Lu and Jinyi Xu*. Discovery of potential anti-inflammatory drugs: diaryl- 1,2,4-triazoles bearing N-hydroxyurea moiety as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase. Org. Biomol. Chem., 2014,12, 2114-2127. (IF 3.487)
  18.Chaolei Wang, Guoxiang Wei, Xue Yang, Hequan Yao, Jieyun Jiang, Jie Liu*, MingqinShen, Xiaoming Wu, Jinyi Xu*. First total synthesis of antihypertensive natural products S-(+)-XJP and R-(−)-XJP. Org. Biomol. Chem., 2014,12, 7338-7344. (IF 3.487)
  19.Jichao Chen, WenliDuan, RenrenBai, Hequan Yao, Jing Shang*, Jinyi Xu*. Design, synthesis and antioxidant activity evaluation of novel β-elemene derivatives. Bioorg. Med. Chem.Lett.,2014, 24, 3407–3411.(IF 2.331)
  20.ShengtaoXu, Dahong Li, Lingling Pei, Hong Yao, Chengqian Wang, HaoCai, Hequan Yao, Xiaoming Wu, Jinyi Xu*. Design, synthesis and antimycobacterial activity evaluation of the compounds derived from natural oridonin. Bioorg. Med. Chem. Lett. 2014, 24, 2811-2814. (IF 2.331)
  21.Shengtao Xu, Lingling Pei, Chengqian Wang, Yun-Kai Zhang, Dahong Li, Hequan Yao, Xiaoming Wu, Zhe-Sheng Chen*, Yijun Sun, Jinyi Xu*. Novel hybrids of natural oridonin bearing nitrogen mustards as potential antitumor drug candidates. ACS Med. Chem. Lett. 2014, 5, 797-802. (IF 3.073)
  22.Shengtao Xu, Lingling Pei, Dahong Li, Hong Yao, HaoCai, Hequan Yao, XiaomingWu, Jinyi Xu*. Synthesis and antimycobacterial evaluation of natural oridonin and its enmein-type derivatives. Fitoterapia, 2014,100, 300-306. (IF= 2.216)
  23.Hao Cai, Yu Zhou, Dong Zhang, Jinyi Xu*, Hong Liu*. A Mannich/cyclization cascade process for the asymmetric synthesis of spirocyclic-thioimidazolidineoxindoles. Chem Commun. 2014, 50, 14771-14774. (IF= 6.834)
  24.Hengyuan Zhang, Yiwei Wang, Peiqing Zhu, Jie Liu, ShengtaoXu, Hequan Yao*, Jieyun Jiang, Wencai Ye, Xiaoming Wu, Jinyi Xu*. Design, synthesis and antitumor activity of triterpenoidpyrazine derivatives from 23-hydroxybetulinic acid. Eur. J. Med. Chem.2015, 97, 235-244. (IF= 3.432)
  25.Hengyuan Zhang, Peiqing Zhu, Jie Liu, Yan Lin, Hequan Yao, Jieyun Jiang, Wencai Ye, Xiaoming Wu, Jinyi Xu*. Synthesis, in vitro and in vivo antitumor activity of pyrazole-fused 23-hydroxybetulinic acid derivatives. Bioorg. Med. Chem. Lett., 2015, 25, 728-732. (IF= 2.331)
  26.Hengyuan Zhang, Fangzheng Li, Peiqing Zhu, Jie Liu, Hequan Yao, Jieyun Jiang, Wencai Ye, Xiaoming Wu, Jinyi Xu*. Synthesis and Biological Evaluation of Oxygen-containing Heterocyclic Ring-fused 23-Hydroxybetulinic Acid Derivatives as Antitumor Agents. Chem. Biol. Drug Des., 2015, 2015, 86, 424-431. (IF= 2.507)
  27.Hengyuan Zhang, Peiqing Zhu, Jie Liu, Xue Yang, ShengtaoXu, Hequan Yao*, Jieyun Jiang, Wencai Ye, Xiaoming Wu, Jinyi Xu*.* Synthesis and antitumor activity of novel 3-oxo-23-hydroxybetulinic acid derivatives. Eur. J. Med. Chem. , 2014, 87, 159-167. (IF= 3.432)
  28.Yi Bi, Cong Ma, Hengyuan Zhang, Zhiwen Zhou,yJian Yang,fZhenlei Zhang,fQingguoMeng*, Peter J. Lewis*, Jinyi Xu*.yNovel 3-Substituted Ocotillol-Type Triterpenoid Derivatives as Antibacterial Candidates. Chem. Bio.l Drug. Des., 2014, 84, 489-496. (IF= 2.507)
  29.Jie Liu, Hengyuan Zhang, Peiqing Zhu, Xiaoming Wu, Hequan Yao, Wencai Ye, Jieyun Jiang, Jinyi Xu*. Synthesis and biological evaluation of ambradiolic acid as an inhibitor of glycogen phosphorylase. Fitoterapia, 2015, 100, 50-55. (IF= 2.216)
  30.Chaolei Wang, Zheng Wu, Jia Wang, Jie Liu*, Hequan Yao, Aijun Lin, Jinyi Xu*. An efficient synthesis of 4-isochromanones viaParham-type cyclization with Weinreb amide. Tetrahedron. 2015, 71, 8172-8177. (IF= 2.641)
  31.Renren Bai, Xiaoming Wu*, Jinyi Xu*. Currentnatural products with antihypertensive activity. Chin. J. Na.t Med. 2015,13,721-729. (IF= 1.114)
  32.Jichao Chen, Wenlong Li, Hequan Yao*, Jinyi Xu*. Insights into drug discovery from natural products through structural modification. Fitoterapia. 2015, 103, 231-241. (IF= 2.345)
  33.Chaolei Wang, Zheng Wu, HaoCai, ShengtaoXu, Jie Liu, Jieyun Jiang, Hequan Yao, Xiaoming Wu*, Jinyi Xu*. Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors. Bioorg. Med. Chem. Let. 2015, 25, 5212-5216. (IF= 2.331)
  34.Xiao Sheng, Kai Hua, Chunyu Yang, Xiaoli Wang, Hui Ji, Jinyi Xu *, Zhangjian Huang *, Zhang Yihua*. Novel hybrids of 3-n-butylphthalide and edaravone: Design, synthesis and evaluations as potential anti-ischemic stroke agents. Bioorg. Med. Chem. Let .2015, 25, 3535-3540. (IF= 2.42)
  35.Zan Li, Zhaoliang Li, Yunwei Lin, Zhaoqing Meng, Gang Ding, Liang Cao, Na Li, Wenjun Liu, Wei Xiao*, Xiaoming Wu*, Jinyi Xu*. Synthesis and Biological Evaluation of Strictosamide Derivatives with Improved Antiviral and Antiproliferative Activities. Chem. Biol. Drug.Des. 2015, 86, 523-530. (IF= 2.485)
  36.Yun-Kai Zhang, Heng-Yuan Zhang, Guan-Nan Zhang, Yi-Jun Wang,Rishil J. Kathawala, Rui Si, Bhargav A. Patel, Jinyi Xu* and Zhe-Sheng Chen*. Semi-synthetic ocotillol analogues as selective ABCB1-mediated drug resistance reversal agents. Oncotarget, 2015, 27, 24277-24290.  (IF= 6.63)
  37.Wei Yin, Lan Li, Zhangjian Huang, Jing Ji, Jiangen Fang, Xiaoli Wang, Hui Ji, Sixun Peng, , Jinyi Xu*, Yihua Zhang *. Discovery of a ring-opened derivative of 3-n-butylphthalide bearing NO/H2S-donating moieties as a potential anti-ischemic stroke agent. Eur. J. Med. Chem. 2016, 115, 369-380. (IF= 3.902)
  38.Shengtao Xu, Guangyu Wang, Yan Lin, Yanju Zhang, Lingling Pei, Hong Yao, Mei Hu, Yangyi Qiu, Zhangjian Huang Yihua, Zhang *, Jinyi Xu*. Novel anticancer oridonin derivatives possessing a diazen-1-ium-1,2-diolate nitric oxide donor moiety: Design, synthesis, biological evaluation and nitric oxide release studies. Bioorg. Med. Chem. Let. 2016, 26, 2795-2800. (IF= 2.486)
  39.Shengtao Xu, Shanshan Luo, Hong Yao, Hao Cai, Xiaoming Miao, Fang Wu, Donghua Yang, Xiaoming Wu, Weijia Xie, Hequan Yao *, Zhesheng Chen, Jinyi Xu*. Probing the Anticancer Action of Oridonin with Fluorescent Analogues: Visualizing Subcellular Localization to Mitochondria. J. Med. Chem. 2016, 59, 5022-5034. (IF= 5.589)
  40.Hao Cai, Xiaojing Huang, Shengtao Xu, Hao Shen, Pengfei Zhang, Yue Huang, Jieyun Jiang, Yijun Sun, Bo Jiang , Xiaoming Wu*, Hequan Yao, Jinyi Xu*. Discovery of novel hybrids of diaryl-1,2,4-triazoles and caffeic acid as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase for cancer therapy. Eur. J. Med. Chem. 2016, 108, 89-103. (IF= 3.902)
  联系方式
  E-mail:jinyixu@china.com;  jinyixu@cpu.edu.cn


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