XU, YUNGEN

Release date:2016-05-17  Release:


XU, YUNGEN

Professor of Medicinal Chemistry

Director of Department of Medicinal Chemistry

School of Pharmacy

Phone: 86-25-83271244

Email: xyg@cpu.edu.cn

Research Summary

Professor XU’s research mainly focuses on three main areasFirst, design and synthesis of novel anti-tumor and anti-inflammatory drugs by application of bioisosterism and scaffold hopping. Second, druggability optimization of bioactive natural products through structural modification. Third, study on new process of drug synthesis.

Education

2000     Ph.D., Medicinal Chemistry, China Pharmaceutical University

1990     M.S., Medicinal Chemistry, China Pharmaceutical University

1987     B.S., Medicinal Chemistry, China Pharmaceutical University

Academic Experience

2005-      Professor of Medicinal Chemistry, China Pharmaceutical University

1999-2005  Associate Professor of Medicinal Chemistry, China Pharmaceutical University

1990-1999  Lecturer of Medicinal Chemistry, China Pharmaceutical University

Awards and Honors

2014   the 6th Top Ten Outstanding Patent Inventor in Jiangsu Province, Intellectual Property Office of Jiangsu Province, Jiangsu Provincial Department of Science and Technology.

Publications (since 2013)

(1) Qiu-fang Chen, Yun-Zhan Li, Xin-Hui Wang, You-Rui Su, Shuang Cui, Ming-Xing Miao, Zhen-Zhou Jiang, Mei-Ling Jiang, Ai-Dou Jiang, Xiang Chen, Yun-Gen Xu*, Guo-Qing Gong*. Evaluating antithrombotic activity of HY023016 on rat hypercoagulable model. European Journal of Pharmacology. 781:190–197, 2016.

  1. Fan-Wei Peng, Ji Xuan, Ting-Ting Wu, Jia-Yu Xue, Zi-Wei Ren, Da-Ke Liu, Xiu-Qi Wang, Xin-Hang Chen, Jia-Wei Zhang, Yun-Gen Xu*, Lei Shi*. Design, synthesis and biological evaluation of N-phenylquinazolin-4-amine hybrids as dual inhibitors of VEGFR-2 and HDAC. Eur. J. Med. Chem., 109:1-12, 2016.

  2. Qihua Zhu, Feng Nie, Jingjie Feng, Yuyan Li, Xuyan Wang, Yungen Xu*.      Palladium-catalyzed Synthesis of Novel O-Heterocycles by Domino Suzuki Coupling-Michael Addition Reaction. J. Heterocyclic Chem., 53(3):919-923, 2016.

  3. Rui Xiong, Jing Sun, Kun Liu, Yungen Xu, Shuying He*. Effect of CPU-XT-008, a combretastatin A-4 analogue, on the proliferation, apoptosis and expression of vascular endothelial growth factor and basic fibroblast growth factor in human umbilical vein endothelial cells. Oncology Lett., 11(1):491-499, 2016.

  4. Xu Zhang, Qian Ba, Zhanni Gu, Diliang Guo, Yu Zhou, Yungen Xu, Hui Wang*, Deju Ye*, Hong Liu*. Fluorescent Coumarin–Artemisinin Conjugates as Mitochondria-Targeting Theranostic Probes for Enhanced Anticancer Activities. Chemistry - A Eur. J., 21(48):17415-17421, 2015.

  5. Qihua Zhu, Xueyan Wang, Yan Hu, Xiaorong He, Guoqing Gong, Yungen Xu*. Discovery and SAR study of 2-(1-propylpiperidin-4-yl)-3H-imidazo[4,5-c]pyridine-7-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1) for the treatment of cancer. Bioorg. Med. Chem., 23(20): 6551-6559, 2015.

  6. Dongxing Chen, Shaochi Wang, Xiaojuan Diao, Qihua Zhu*, Huiliang Shen, Xueqing Han, Yiwei Wang, Guoqing Gong, Yungen Xu*. Design, synthesis and antithrombotic evaluation of novel dabigatran etexilate analogs, a new series of non-peptides thrombin inhibitors. Bioorg. Med. Chem., 23(23):7405-16, 2015.

  7. Haiping Zhou, Qihua Zhu, Zongjie Gan, Guangping Dong, Yungen Xu*. Synthesis and biological evaluation of novel laropiprant derivatives as potential antiallergic agents. Med. Chem. Res., 24(11): 3920-3931, 2015.

  8. Qihua Zhu£, Junwei Wang£, Xueguo Bian, Lingzhi Zhang, Ping Wei, and Yungen Xu*. Novel Synthesis of Antiobesity Drug Lorcaserin Hydrochloride. Org. Process Res. Dev., 19 (9), 1263–1267, 2015.

  9. 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.

  10. Qihua Zhu1, Dezhong Ji1, Tingting Liang, Xueyan Wang, Yungen Xu*. Efficient Palladium-Catalyzed C−H Fluorination of C(sp3)−H Bonds: Synthesis of β-Fluorinated Carboxylic Acids. Org. Lett., 17, 3798−3801, 2015.

  11. 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(8): 595–605, 2015.

  12. 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.

  13. 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, 6659-671, 2015.

  14. 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), 1–9, 2015.

  15. 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.

  16. 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.

  17. 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. J. Chromatogr. B., 973C:110–119, 2014.

  18. 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.

  19. 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.

  20. 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.

  21. 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.

  22. 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.

  23. 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.

  24. 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):1993-1996, 2013.

  25. 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.

  26. 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.

  27. 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(7): 2089-2092, 2013.