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School of Pharmaceutical Sciences Shandong University, Jinan 250012, China
Tel/Fax: 86-531-88382009
Email: guisenzhao@sdu.edu.cn |
Present Position:
Professor of Medicinal Chemistry
Director of Drug Discovery Laboratory，School of Pharmaceutical Sciences，Shandong University
Education Background:
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
Professional Experience:
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
Teaching Courses:
Medicinal Chemistry, Drug design and discovery, Chemical Biology
Research Interests:
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:
Currently Active:
The National Natural Science Foundation of China (Grant No. 21072115; No. 21272140)
Shandong Provincial Natural Science Foundation (Grant No. ZR2011HM042)
Grants Completed:
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)
Patents:
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)
Recent Publications:
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.
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