YOU, QIDONGProfessor of Medicinal ChemistryDirector of Jiangsu Key Laboratory of Drug Design and OptimizationSchool of PharmacyPhone: 86-25-83271351Email: youqd@cpu.edu.cnResearch SummaryProfessor YOU’s research interesting is on the drug design and synthesis, the action mechanism of drug molecular and new drug research and development. The recent research focuced on two main fields: 1) natural product and its derivatives, structure-activities relationships, structure modification simplification and optimization; 2) Bioactive compound discovery for targeting on the protein structure and function, such as,  protein-protein interaction, protein degradation and the new drug design for cancer.Education1989       Ph.D., Medicinal Chemistry, Shanghai Institute of Pharmaceutical Industry1985       M.S.,  Medicinal Chemistry, Shanghai Institute of Pharmaceutical Industry1982       B.S.,   Medicinal Chemistry，Nanjing College of Pharmacy (the former of China Pharmaceutical University)Academic Experience1994-      Professor of Medicinal Chemistry, China Pharmaceutical University, Associate Dean of School of Pharmacy (1995 to 2009), Dean of School of Pharmacy (2009 to 2015),1994-1995  Senior Visiting Scholar, University of Strathclyde, UK1990-1994 Associate Professor of Medicinal Chemistry, China Pharmaceutical University,Awards and Honors1994      Henry Fok outstanding young teachers Award, Henry Fok Education Foundation2013       Wu Jieping-Paul Janssen Award in medicine & Pharmacy, Ministry of Health2016       First prize for scientific and technological progress of Jiangsu，Jiangsu Province 2012       Second prize for scientific and technological progress of Jiangsu，Jiangsu Province2007       Second prize for scientific and technological progress of Jiangsu，Jiangsu Province2014       Second prize for National Teaching Achievement Award, Ministry of Education2009       Second prize for National Teaching Achievement Award, Ministry of Education PublicationsBooks (selected):Chiral Drugs: Chemistry and Biological Action. Ed by Guo-Qiang Lin, Qi-Dong You and Jie-Fei Cheng, John Wiley & Sons, Inc. Hoboken, 2011Research and Evaluation of Chiral Drugs, Ed by Qi-Dong You and Guo-Qiang Lin, Chemical Industry Press. Beijing, 2011Medicinal Chemistry, 3rd edition, Ed by Qi-Dong You, Chemical Industry Press. Beijing, 2015Papers and Articles (selected)Palladium(II)-Catalyzed C-H Bond Activation/C-C Coupling/Intramolecular Tsuji-Trost Reaction Cascade: Facile Access to 2H-Pyranonaphthoquinones. Bian, Jinlei; Qian, Xue; Wang, Nan; Mu, Tong; Li, Xiang; Sun, Haopeng; Zhang, Lianshan; You, Qidong; Zhang, Xiaojin. Org Lett. 2015, 17 (14):3410–3413Structure-Activity and Structure-Property Relationship and Exploratory in vivo Evaluation of the Nanomolar Keap1-Nrf2 Protein-Protein Interaction Inhibitor. Zhengyu Jiang, Lili Xu, Mengchen Lu, Zhiyun Chen, Zhenwei Yuan, Xiaoli Xu, Xiaoke Guo,Xiaojin Zhang, Haopeng Sun, Qi-Dong You.J. Med. Chem.,2015, 58 (16):6410–6421Discovery and Modification of in vivo active Nrf2 Activators with 1, 2, 4-oxadiazole Core: Hits Identification and Structure-Activity Relationship Study. Xu, Lili; Zhu, Junfeng; Xu, Xiaoli; Zhu, Jie; Li, Li; Xi, Meiyang; Jiang, Zhengyu; Zhang, Mingye; Liu, Fang; Lu, Mengchen; Bao, Qichao; Zhang, Chao; Wei, Jinlian; Zhang, Xiaojin; You, Qi-Dong; Sun, Haopeng. J Med Chem.2015, 58 (14), pp 5419–5436Novel 5-carboxy-8-HQ based histone demethylase JMJD2A inhibitors: Introduction of an additional carboxyl group at the C-2 position of quinoline. Feng T, Li D, Wang H, Zhuang J, Liu F, Bao Q, Lei Y, Chen W, Zhang X, Xu X, Sun H, You Q, Guo X.Eur J Med Chem. 2015, 105:145-155.Binding thermodynamics and kinetics guided optimization of potent Keap1-Nrf2 peptide inhibitors. Lu, M.-C.; Chen, Z.-Y.; Wang, Y.-L.; Jiang, Y.-L.; Yuan, Z.-W.; You, Q.-D. *; Jiang, Z.-Y. *RSC Advances 2015, 5:85983-85987Identification of Novel JMJD2A Inhibitor Scaffold Using Shape and Electrostatic Similarity Search Combined with Docking Method and MM-GBSA Approach. Feng, T. T.; Chen, W. L.; Li, D. D.; Lin, H. Z.; Liu, F.; Bao, Q. C.; Lei, Y. H.; Zhang, X. J.; Xu, X. L.; Guo, X. K.; You, Q. D.*; Sun, H. P.*RSC Advances,2015, 5:82936-82946.Discovery of NAD(P)H:quinone oxidoreductase 1 (NQO1) inhibitors with novel chemical scaffolds by shape-based virtual screening combined with cascade docking. Bian, J.; Qian, X.; Deng, B.; Xu, X.; Guo, X.; Wang, Y.;* Li, X.; Sun, H.; You, Q.;* Zhang, X.*RSC Advances, 2015, 5 (61), 49471-49479. Affinity-based fluorescence polarization assay for high-throughput screening of prolyl hydroxylase 2 inhibitors. Lei, Y.; Hu, T.; Wu, X.; Wu, Y.; Bao, Q.; Zhang, L.; Xia, H.; Sun, H.; You, Q.;* Zhang, X.* ACS Med. Chem. Lett., 2015, 6 (12), 1236−1240. (IF=3.120)CPUY201112, a novel synthetic small-molecule compound and inhibitor of heat shock protein Hsp90, induces p53-mediated apoptosis in MCF-7 cells. Xiao-Li Xu, Qi-chao Bao, Jian-Min Jia, Fang Liu, Xiao-Ke Guo, Ming-ye Zhang, Jin-lian Wei, Meng-chen Lu, Li-li Xu, Xiao-Jin Zhang, Qi-Dong You & Hao-Peng Sun.Scientific Reports2016, 6:19004A systematic molecular dynamics approach to the study of peptide Keap1-Nrf2 protein-protein interaction inhibitors and its application to p62 peptides. Lu, Meng-Chen, ,Yuan, Zhen-Wei,  Jiang, Yong-Lin, Chen, Zhi-Yun, You, Qi-Dong, Jiang, Zheng-Yu.Mol. BioSyst.,2016,12(4):1378-1387

YANG, PENGYANG, PENGProfessor of Medicinal ChemistryEmail: pengyang@cpu.edu.cnResearch SummaryProfessor YANG’s research focuses on identification of new drug targets and novel leading compounds, drug design and chemical synthesis, the action mechanism of drug molecular, and new drug research and development. The recent research focused on three main fields: (1) natural products and small molecules, structure-activity relationship studies, chemical modification and optimization, bioactivity evaluation at cell- and animal-levels; (2) discovery of new drug targets and novel leading compounds through unique virtual screening; (3) interaction studies between small molecule and protein target, mechanism studies at molecule level.Education2008: Ph. D., Medicinal Chemistry, Chinese Academy of Medical Sciences and Peking Union Medical College, Tsinghua University2005: M.S., Medicinal Chemistry, Chinese Academy of Medical Sciences and Peking Union Medical College2002: B.S., Pharmacy, School of Pharmacy, Shandong University  Academic Experience2018.03-present: Professor of Medicinal Chemistry, China Pharmaceutical University2017.08-2018.02: Associate Director of Medicinal Chemistry, Bioduro (Shanghai) Co., Ltd2015.11-2017.07: Assistant Professor, University of Pittsburgh, USA2011.06-2015.10: Post-doctoral Research Associate, University of Pittsburgh, USA2008.08-2011.05: Senior Scientist & Group Leader, Bioduro (Beijing) Co., LtdAwards and Honors2015      Outstanding Research Achievements Award2007      “Professor Satoshi Omura” Award2004      “Academician Zhen Yongsu” AwardPublicationsCha-Molstad H.#, Yu J.#, Feng Z.#, Lee S.#, Kim J.#, Yang P.# (equal contribution), Yoo Y., Hwang J., McGuire T., Shim S., Song H., Ganipisetti S., Wang N., Jang J., Lee M., Kim S., Lee K., Hong J., Ciechanover A., Mook-Jung I., Xie X-Q*, Kwon Y.*, and Kim B.* p62/SQSTM1 Is an Autophagic Inducer Mediating Crosstalk between the Ubiquitin-Proteasome System and Autophagy. Nat Commun. 2017, 8(1):102.Teramachi J.#, Silberma R.#, Yang P.# (equal contribution), Zhao W., Mohammad K., Guo J, Anderson JL, Zhou D, Feng R, Myint KZ, Maertz N, Beumer JH, Eiseman JL, Windle JJ, Xie XQ*, Roodman GD*, Kurihara N*.. Blocking the ZZ domain of sequestosome1/p62 suppresses myeloma growth and osteoclast formation in vitro and induces dramatic bone formation in myeloma-bearing bones in vivo. Leukemia, 2016; 30(2):390-8.Gao Y#, Yang P# (equal contribution), Shen H#, Yu H, Song X, Zhang L, Zhang P, Cheng H, Xie Z, , Dong F, Ma S, Ji Q, Bartlow P, Ding Y, Wang L, Liu H, Li Y, Cheng H, Miao W, Yuan W, Yuan Y, Cheng T*, Xie XQ*: Small-molecule inhibitors targeting INK4 protein p18(INK4C) enhance ex vivo expansion of haematopoietic stem cells. Nat Commun. 2015, 6:6328.Yang P., Wang L., Feng R., Almehizia A.A., Tong Q., Myint K.Z., Ouyang Q., Alqarni M.H., Wang L., Xie X.Q.* Novel triaryl sulfonamide derivatives as selective cannabinoid receptor 2 inverse agonists and osteoclast inhibitors: discovery, optimization, and biological evaluation. J. Med. Chem. 2013, 14; 56 (5):2045-58.Yang, P.#; Myint, K. Z.#; Tong, Q.; Feng, R.; Cao, H.; Almehizia, A. A.; Bartlow, P.; Gertsch, J.; Teramachi, J.; Kurihara, N.; Roodman, G. D.; Cheng, T.; Xie, X. Q.* Lead Discovery, Chemistry Optimization and Biological Evaluation Studies of Novel Bi-amide Derivatives as CB2 Receptor Inverse Agonists and Osteoclast Inhibitors. J. Med. Chem. 2012, 55, 9973-9987. 

XU,YUNGENProfessor of Medicinal ChemistryDirector of Department of Medicinal ChemistrySchool of PharmacyPhone: 86-25-83271244Email: xyg@cpu.edu.cnResearch SummaryProfessor XU’s research mainly focuses on three main areas：First, 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.Education2000     Ph.D., Medicinal Chemistry, China Pharmaceutical University1990     M.S., Medicinal Chemistry, China Pharmaceutical University1987     B.S., Medicinal Chemistry, China Pharmaceutical UniversityAcademic Experience2005-      Professor of Medicinal Chemistry, China Pharmaceutical University1999-2005  Associate Professor of Medicinal Chemistry, China Pharmaceutical University1990-1999  Lecturer of Medicinal Chemistry, China Pharmaceutical UniversityAwards and Honors2014   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.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.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.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.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.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.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.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.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.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.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.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.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.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.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.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.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.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.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.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.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.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.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.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.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.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.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.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.

XU, JINYIProfessorDepartment of Medicinal ChemistrySchool of PharmcyPhone: 86-25-83271299Email: jinyixu@cpu.edu.cnResearch SummaryProfessor 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.Education2001 Ph.D. Medicinal ChemistryChina Pharmaceutical University1991 M.S. Medicinal ChemistryChina Pharmaceutical University1986 B.S. Pharmacology China Pharmaceutical UniversityAcademic Experience2006-      Professor of Department of Medicinal ChemistryAdviser of Ph. D. 2000-2005 Associate Professor of Department of Medicinal Chemistry 1993-1999  Lecturer of Department of Medicinal Chemistry PublicationsBooksPharmaceutical 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.