Professor
Department of Medicinal Chemistry
School of Pharmcy
Phone: 86-25-83271299
Email: jinyixu@cpu.edu.cn
Research Summary
Professor XU’s research focuses on the design and synthesis of novel cardiovascular drugs and studies on the structural modification and biological evaluation of natural products.
She joined the cardiovascular drugs research group, involving in discovery non-peptide angiotensin II AT1 receptor antagonists and novel antihypertensive drugs. She also joined the antineoplastic agents research group, involving in the modification of anticancer compounds from plants and synthesis of novel derivatives of natural products, such as 23-hydroxy betulinic acid, 7,8-dihydroxy-3-methyl-isochromanone, oridonin,berberine, evodiamine,elemene and study on their biological activities, action of mechanisms as well as the structure activity relationships. She also joined the research group of novel anti-inflammatory agents, involving in the research and development of COX-2 inhibitors and dual cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) inhibitors as well as the related anti-tumor agents.
Education
2001 Ph.D. Medicinal Chemistry
China Pharmaceutical University
1991 M.S. Medicinal Chemistry
China Pharmaceutical University
1986 B.S. Pharmacology
China Pharmaceutical University
Academic Experience
2006- Professor of Department of Medicinal Chemistry
Adviser of Ph. D.
2000-2005 Associate Professor of Department of Medicinal Chemistry
1993-1999 Lecturer of Department of Medicinal Chemistry
Publications
Books
Pharmaceutical Chemistry Experiments. Medical Sciences and Technology Press, 1999, Dec.
Medicinal Chemistry. Chemistry and Industry Press, 2006, July.
Medicinal Chemistry. Science and Technology of Literature Press,2005, Feb.
Medicinal Chemistry. Dongnan University Press,2008, Oct.
Papers and Articles
(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.
(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 acidderivatives as novel inhibitors of glycogen phosphorylase. Bioorg. & Med. Chem. Lett., 2009, 19: 6966–6969.
(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.
(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.
(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.
(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.
(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.
(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.
(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.
(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.
(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.
(12) Renren Bai, Zhen Wei, Jie Liu, Weijia Xie, Hequan Yao, Xiaoming Wu*, Jieyun Jiang, Qiujuan Wang and JinyiXu*. 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.
(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.
(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.
(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.
(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.
(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.
(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.
(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.
(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.
(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.
(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.
(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.
(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.
(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.
(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.
(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.
(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.
(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.
(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.
(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.
(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.
(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.
(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, 86, 424-431.
(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.
(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.
(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, 27, 24277-24290.
(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, 71,8172-8177.
(39) Hao Cai, Xiaojing Huang, Shengtao Xu, Hao Shen, Pengfei Zhang,Yue Huang, Jieyun Jiang, Yijun Sun, Bo Jiang, Xiaoming Wu*, Hequan Yao,Jingyi 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.
(40) Shengtao Xu, Shanshan Luo, Hong Yao, Hao Cai, Xiaoming Miao, Fang Wu*, Dong-Hua Yang, Xiaoming Wu, Weijia Xie, Hequan Yao, Zhe-Sheng Chen, Jinyi Xu*. Probing the Anticancer Action of Oridonin with Fluorescent Analogues: Visualizing Subcellular Localization to Mitochondria. J Med Chem, 2016, accepted,doi: 10.1021/acs.jmedchem.6b00408.
