中国药科大学

徐进宜：药学博士，教授，博导，中国药科大学药学院药物化学教研室副主任。

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（硕士招生方向）

2. 针对重大疾病的创新药物研究（博士招生方向）

1986年毕业于中国药科大学，留校任教29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70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 Chemistry，European Journal of Medicinal Chemistry, Bioorganic & Medicinal Chemistry等国际杂志特约审稿人。

研究经历包括：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；选择性环氧化酶II抑制剂的研究；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。

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。

近期研究成果代表性SCI论文（总影响因子大于115），均为通讯作者。

(1)Jie Liu, Hao Ren, Jinyi Xu*, Renren Bai, 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)Peiqing Zhu, Yi Bi, Jinyi Xu*, Zan Li, Jun Liu, Luyong Zhang, Wencai Ye, Xiaoming Wu*. Terpenoids. III: Synthesis and biological evaluation of 23-hydroxybetulinic acid derivatives as novel inhibitors of glycogen phosphorylase. Bioorg. & Med. Chem. Lett., 2009, 19: 6966–6969. (IF 2.661)

(3)Bo Jiang, Yi Zeng, Jinyi Xu*, Yongna Zhang, Qiujuan Wang, Niyue Sun, Tao Lu, and Xiaoming Wu. Design, Synthesis, and Biological Evaluation of 1, 5-Diarylsubstitued-1, 2, 4-triazole Derivatives as Selective Cyclooxygenase-2 Inhibitors. Archiv der Pharmazie, 2010, 9:500-508. (IF 1.708)

(4)Yiyun Wang, Ziyuan Li, Yue Huang, Changhua Tang, Xiaoming Wu, Jinyi Xu*, Hequan Yao*. Copper (II)-catalyzed oxidation of 4-carboxythiazolines and 4-carboxyoxazolines to 4-carboxythiazoles and 4-carboxyoxazoles. Tetrahedron. 2011, 67, 7406-7411. (IF 3.025)

(5)Shang Li, Hequan Yao, Jinyi Xu*, Sheng Jiang*. Synthetic Routes and Biological Evaluation of Largazole and Its Analogues as Potent Histone Deacetylase Inhibitors. Molecules. 2011, 16, 4681-4694. (IF 2.386)

(6)Lei Wang, Dahong Li, Yihua Zhang*, Jinyi Xu*. Recent progress in the development of natural ent-kaurane diterpenoids with anti-tumor activity. Mini-Rev. Med. Chem. 2011, 11, 910-919. (IF 2.528)

(7)Chao Lei Wang, Bing-Feng Sun*, Shu-Guang Chen, Rui Ding, Guo-Qiang Lin*, Jin-yi 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)

(8)Dahong Li, Lei Wang, Hao Cai, Yihua Zhang*, Jinyi Xu*. Synthesis and biological evaluation of novel furozan-based nitric oxide-releasing derivatives of oridonin as potential anti-tumor agents. Molecules, 2012, 17, 7556-7568. (IF 2.386)

(9)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)

(10)Yi Bi, Jinyi Xu*, Fei Sun, Xiaoming Wu*, Wencai Ye, Yijun Sun and Wenwen Huang.  Synthesis and biological activity of 23-hydroxybetulinic acid C-28 ester derivatives as antitumor agent candidates. Molecules, 2012, 17(8): 8832-8841. (IF 2.386)

(11)Renren Bai, Xue Yang, Yao Zhu, Zhiwen Zhou, Weijia Xie, Hequan Yao, Jieyun Jiang, Jie Liu*, Mingqin Shen, 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)

(12)Renren Bai, Zhen Wei, Jie Liu, Weijia Xie, 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)

(13)Renren Bai, Jie Liu, Yao Zhu, Xue Yang, Chen Yang, Lingyi Kong, Xiaobing Wang, Hengyuan Zhang, Hequan Yao, Mingqin Shen, 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. (IF 2.661)

(14)Lei Wang, Dahong Li, Shengtao Xu, 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. (IF 3.499) 

(15)Xiaoli Wang, Qian Zhao, Xuliang Wang, Tingting Li, Yisheng Lai, Sixun Peng, Hui Ji, Jinyi Xu* and 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)

(16)Dahong Li, Hao Cai, 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. (IF 3.499)

(17)Xiaoli Wang, Linna Wang, Zhangjian Huang, Tingting Li, Hui Ji, Jinyi Xu*, Yihua Zhang*. Synthesis and biological evaluation of nitric oxide releasing derivatives of  6-amino-3-n-butyl phthalide as potential antiplatelet agents. Bioorg Med Chem Lett, 2013, 1985-1988. (IF 2.921)

(18)Renren Bai, Xue Yang, Wen Hong, Yiqun Tang, Hequan Yao, Jieyun Jiang, Jie Liu, Mingqin Shen, 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)

(19)Shengtao Xu, 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)

(20)Xiaoli Wang, Linna Wang, Tingting Li, Zhangjian Huang, Yisheng Lai, Hui Ji, 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)

(21)Dahong Li, Shengtao Xu, Hao Cai, 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)

(22)Dahong Li, Shengtao Xu, Hao Cai, 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)

(23)Ziwen Zhou, Cong Ma, Hengyuan Zhang, Y Bi, Xia Chen, Hua Tian, Xiaoni Xie, Qingguo Meng, Peter John Lewis*, Jinyi Xu*. Synthesis and Biological Evaluation of Novel Ocotillol-Type Triterpenoid Derivatives as Antibacterial Agents. Eur. J. Med. Chem. 2013, 68, 444-453. (IF 3.499)

(24)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)

(25)Chaolei Wang, Guoxiang Wei, Xue Yang, Hequan Yao, Jieyun Jiang, Jie Liu*, Mingqin Shen, Xiaoming Wu and Jinyi Xu*. First total synthesis of antihypertensive natural products S-(+)-XJP and R-(−)-XJP. Org. Biomol. Chem., 2014, 12, 7338-7344. (IF 3.487)

(26)Jichao Chen, Wenli Duan, Renren Bai, 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)

(27)Shengtao Xu, Dahong Li, Lingling Pei, Hong Yao, Chengqian Wang, Hao Cai, 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)

(28)Novel hybrids of natural oridonin bearing nitrogen mustards as potential antitumor drug candidates. Shengtao Xu, Lingling Pei, Chengqian Wang, Yun-Kai Zhang, Dahong Li, Hequan Yao, Xiaoming Wu, Zhe-Sheng Chen*, Yijun Sun, Jinyi Xu*. ACS Med. Chem. Lett. 2014, 5, 797-802. (IF 3.073)

(29)Synthesis and antimycobacterial evaluation of natural oridonin and its enmein-type derivatives. Shengtao Xu, Lingling Pei, Dahong Li, Hong Yao, Hao Cai, Hequan Yao, Xiaoming Wu, Jinyi Xu*. Fitoterapia 2014, 100, 300-306. (IF 2.216)

(30)Yi Bi, Cong Ma, Hengyuan Zhang, Zhiwen Zhou,Jian Yang,Zhenlei Zhang,Qingguo Meng*, Peter J. Lewis*, Jinyi Xu*.Novel 3-Substituted Ocotillol-Type Triterpenoid Derivatives as Antibacterial Candidates. Chem. Bio.l Drug. Des., 2014, 84, 489-496. (IF 2.507)

(31)A Mannich/cyclization cascade process for the asymmetric synthesis of spirocyclic thioimidazolidineoxindoles. Hao Cai, Yu Zhou, Dong Zhang, Jinyi Xu*, Hong Liu*. Chem Commun. 2014, 50, 14771-14774. (IF 6.834)

(32)Hengyuan Zhang, Yiwei Wang, Peiqing Zhu, Jie Liu, Shengtao Xu, Hequan Yao*, Jieyun Jiang, Wencai Ye, Xiaoming Wu, Jinyi Xu*. Design, synthesis and antitumor activity of triterpenoid pyrazine derivatives from 23-hydroxybetulinic acid. Eur. J. Med. Chem. 2015, 97, 235-244. (IF 3.432)

(33)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)

(34)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, doi: 10.1111/cbdd.12543. (IF 2.507)

(35)Hengyuan Zhang, Peiqing Zhu, Jie Liu, Xue Yang, Shengtao Xu, 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)

(36)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)

(37)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, online. (IF 6.63)

(38)Chaolei Wang, Zheng Wu, Jia Wang, Jie Liu*, Hequan Yao, Aijun Lin, Jinyi Xu*. An efficient synthesis of 4-isochromanones via Parham-type cyclization with Weinreb amide. Tetrahedron, 2015, doi:10.1016/j.tet.2015.08. 028. (IF 2.641)

联系方式

E-mail：jinyixu@china.com;  jinyixu@cpu.edu.cn