School of Pharmaceutical Sciences Shandong University, Jinan 250012, China
Professor of Medicinal Chemistry
Director of Drug Discovery Laboratory，School of Pharmaceutical Sciences，Shandong University
2006.12: Ph D, School of Pharmaceutical Sciences，Shandong University 1988.09-1991.03: M. Sci., College of Pharmacy, Shandong Medical University
1985.09-1986.08: Visiting Scholar, Department of Medicinal Chemistry, Beijing Medical University
1979.06-1983.09: B. Sci., College of Pharmacy, Shandong Medical University
2001.09- Present: Professor, Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University
2011.05-2011.08: Senior Visiting Fellow, Mount Sinai School of Medicine, The United States of America
1998.04-1999.09: Visiting Scientist, The University of Iowa, United States of America
1997.01-2001.08: Associate Professor, Department of Medicinal Chemistry, College of Pharmacy, Shandong Medical University
1983.07 -1996.12: Teaching Assistant, Lecturer, Department of Medicinal Chemistry, College of Pharmacy, Shandong Medical University
Medicinal Chemistry, Drug design and discovery, Chemical Biology
Rational design, synthesis and discovery of anticancer agents, particularly targeting GSTP1-1, AKT and androgen receptor.
Antiviral and anti-aids drugs. Discovery and development of HIV-1 integrase inhibitors as anti-AIDS drug.
Research Grant Support:
The National Natural Science Foundation of China (Grant No. 21072115; No. 21272140)
Shandong Provincial Natural Science Foundation (Grant No. ZR2011HM042)
National Major Projects of Science and Technology for Drug Innovation of China (Grant No. 2009ZX09103-116)
The National Natural Science Foundation of China (Grant No. 20872082; No. 20672069)
Shandong Provincial Natural Science Foundation (Grant No. Y2007C060)
1. The synthesis and HIV intergrase inhibitory activity of caffeoyl naphthalenesulfonamide derivatives (CN 03138909.0)
2. The synthesis of alpha, beta-unsaturated carbonyl derivatives and the ability to inhibit GSTπ activity (CN 200510043573.3).
3. The synthesis and application of amide-containing diketacides (CN 200710016183.6)
4. The synthesis and application of five membered heterocyclic compounds (CN 200710015199.5)
5. The synthesis and application of alpha, beta-unsaturated carbonyl derivatives with 1, 2, 4-oxdiazole(CN 201010215382.1)
6. The synthesis and application of indoledione derivatives (CN 201010190072.9)
7. The synthesis and application of nitrogen-containing polyhydroxylated aromatics (CN 200810238611.4)
8. The synthesis and application of 4-styrylpyridinium derivatives (CN 201010207655.8)
Ting Li; Guyue Liu; Hongcai Li; Xinmei Yang; Yongkui Jing; Guisen Zhao*. The synthesis of ethacrynic acid thiazole derivatives as glutathione S-transferase pi inhibitors. Bioorg Med Chem, 2012, 20, 2316-2322.
Yang Liu, Yijing Li, Shenghui Yu and Guisen Zhao*. Recent Advances in the Development of Thioredoxin Reductase Inhibitors as Anticancer Agents. Current Drug Targets, 2012, 13, 1432-1444
Shenghui Yu, Linna Zhang, Shifeng Yan, Peng Wang, Tino Sanchez, Frauke Christ, Zeger Debyser, Nouri Neamati, and Guisen Zhao*. Nitrogen-containing polyhydroxylated aromatics as HIV-1 integrase inhibitors: synthesis, structure- activity relationship analysis, and biological activity. J Enzyme Inhib and Med Chem, 2012, 27, 628-640.
Peng Wang, Jianzhen Liu, Hualu Xing, Yang Liu, Wencheng Xie, Guisen Zhao*. Synthesis and anticancer activity of novel 5-(indole-2-yl)-3-substituted 1,2,4-oxadiazoles. Drug Discoveries & Therapeutics. 2012; 6(3):133-139.
Peng Wang, Hualu Xing, Yang Liu, Wencheng Xie and Guisen Zhao*. Methyl 4-benzyloxy-7-methoxy-1- methyl-1H-indole-2-carboxylate. Acta Cryst. 2012; E68, o2480.
P. Wang, L. Zhang, Q. Hao, G. Zhao*. Developments in Selective Small Molecule ATP-Competitive Inhibitors Targeting the Serine/Threonine Kinase Akt/PKB. Mini-Reviews in Medicinal Chemistry, 2011, 11(13): 1093-1107.
Xinmei Yang, Guyue Liu, Hongcai Li, Yun Zhang, Dandan Song, Chunmin Li, Rui Wang, Bo Liu, Wen Liang, Yongkui Jing, Guisen Zhao*. Novel Oxadiazole Analogues Derived from Ethacrynic Acid: Design, Synthesis, and Structure- Activity Relationships in Inhibiting the Activity of Glutathione S-Transferase P1-1 and Cancer Cell Proliferation. J Med Chem, 2010, 53(3): 1015-1022.
Bo Liu, Lei Su, Jingkun Geng, Junjie Liu, Guisen Zhao*. Developments in nonsteroidal antiandrogens targeting the androgen receptor. ChemMedChem, 2010, 5(10):1651-1661.
Shenghui Yu, Sitai Zhao, Chuan Liu, Yuan Zhong, Guisen Zhao*. Synthesis and HIV-1 Integrase Inhibitory Activity of Furanone Derivatives. CHEM RES CHINESE UNIVERSITIES, 2010, 26(2):225-229.
Hongcai Li, Chao Wang, Tino Sanchez, Yanmei Tan, Chunying Jiang, Nouri Neamati, Guisen Zhao*. Amide-containing diketoacids as HIV-1 integrase inhibitors: synthesis, structure-activity relationship analysis, and biological activity. Bioorg Med Chem, 2009, 17(7):2913-2919.
Peng Wang , Chuan Liu , Tino Sanchez , Yuan Zhong , Bo Liu , Junlong Xiong , Nouri Neamati, Guisen Zhao*. Design and synthesis of novel nitrogen- containing polyhydroxylated aromatics as HIV-1 integrase inhibitors from caffeic acid phenethyl ester. Bioorganic & Medicinal Chemistry Letters，2009, 19(16): 4574–4578.
Guisen Zhao, Chao Wang, Chuan Liu and Hongxiang Lou. New Developments in Diketo- Containing Inhibitors of HIV-1 Integrase . Mini-Reviews in Medicinal Chemistry, 2007, 7(7):707-725.
Wang, R.; Li, C.; Song, D.; Zhao, G.; Zhao, L.; Jing, Y. Ethacrynic acid butyl-ester induces apoptosis in leukemia cells through a hydrogen peroxide mediated pathway independent of glutathione S-transferase P1-1 inhibition. Cancer Res, 2007, 67, 7856-7864.
Guisen Zhao, Chuan Liu, Rui Wang, Dandan Song, Xiaobing Wang, Hongxiang Lou and Yongkui Jing. The synthesis of α, β-unsaturated carbonyl derivatives with the ability to inhibit both glutathione S-transferase P1-1 activity and the proliferation of leukemia cells. Bioorganic & Medicinal Chemistry, 2007, 15: 2701–2707.
Guisen Zhao and Xiaobing Wang. Advance in antitumor agents targeting glutathione- S-transferas. Current Medicinal Chemistry, 2006, 13 (12): 1461-1471.