Fu, Lei



Tel: 021-34204791
Email: leifu@sjtu.edu.cn

Lei Fu, Ph.D.

Professor of Medicinal Chemistry
School of Pharmacy
Shanghai Jiao Tong University, Shanghai, 200240, China

Professor Lei Fu received his B.Sc. and M. Sc. degrees in Chemistry from Fudan University, Shanghai, China, and his Ph.D. degree in Chemistry from Stanford University under the direction of Dr. James P. Collman. He joined Pharmacyclics Inc. (then acquired by AbbVie), California in 1998 as a scientist and group leader. He led the drug discovery & development, process research on anti-cancer and anti-cardiovascular diseases. He has been a Summer visiting scholar in the Department of Chemistry, Stanford University since 2009, and a scientific consultant to several pharmaceutical companies.
Dr. Lei Fu has been a Professor of Medicinal Chemistry at Shanghai Jiao Tong University since March of 2007. The research in his group interfaces chemistry and medicine. His principal interests are 1) drug discovery and development; 2) process research on drug API and related substances; 3) traditional Chinese Medicines as botanical cosmeceuticals; 4) medical devices as targeted drug delivery systems and 5) human hibernation studies using biomimetic models of cytochrome c oxidase. Dr. Fu teaches undergraduate and graduate courses, including Principles of Medicinal Chemistry, Comprehensive Pharmacy, Presenting Science, Chemistry and Pharmacology for layman etc.
Dr. Fu is an adjunct Professor at Roosevelt University and Santa Clara University in the US, also an Editor of Bioorganic Chemistry (Elsevier) and Pharmaceutical Fronts (Thieme).
Dr. Fu has over 70 peer-reviewed publications mainly in drug discovery. Several of them were published in Science, PNAS, Chemical Reviews, Angewandte Chemie International Edition, Journal of the American Chemical Research, the Journal of Organic Chemistry and European Journal of Medicinal Chemistry. He holds more than 20 US and China Patents.
Dr. Fu invented two cosmeceutical products containing traditional Chinese medicines (TCMs) and licensed to German companies, Henkel and Beiersdorf, respectively.
Dr. Fu initiated a collaborative research project with Ethiopia Addis Ababa University, Centre for Innovative Drug Development and Therapeutic Trials for Africa (CDT-Africa, supported by the World Bank and State government), on the development of Africa local medicinal herbal and establishment of Africa herbal pharmacopeia.

Lei Fu, Ph.D.

Professor of Medicinal Chemistry
Associate Dean, School of Pharmacy
Shanghai Jiao Tong University, Shanghai, 200240, China

Education/Professional Training
Post doc. Chemistry, Department of Chemistry, Stanford University, Stanford, CA (1998)
Ph.D. Chemistry, Department of Chemistry, Stanford University, Stanford, CA (1997)
M.Sc. Nuclear and Radiochemistry, Fudan University, Shanghai, China (1987)
B.Sc. Chemistry, Fudan University, Shanghai, China (1984)
Positions and Employment
Professor of Medicinal Chemistry (2006.3-present) School of Pharmacy
Shanghai Jiao Tong University
Co-Founder, Director (2005.3-2008.12) ND Pharmaceuticals, Inc.
Shanghai, China
Principal Investigator and Group Leader (1998.11-2005.1) Pharmacyclics, Inc.
Sunnyvale, California., USA
Postdoctoral Research Associate (1997.3-1998.10) Department of Chemistry
Stanford University, California
Invited Scientist (1990.9-1993.8) Department of Chemistry
Free University Berlin, Germany
Lecturer (1987.9-1990.8) Fudan University
Shanghai, China
Other Experience and Professional Memberships
Adjunct Professor (2015.03-) Roosevelt University
College of Pharmacy,
Schaumburg, IL 60173, USA
Adjunct Professor (2013.05-) Santa Clara University
School of Engineering, Bioengineering Department
Santa Clara, California, USA
Visiting Professor (Summers of 2009, 2010 & 2016-) Stanford University
Department of Chemistry
Stanford, California, USA
Consultant & SAB member (2013.9-) Blue Bay Science & Technology Co. Ltd.
Xiamen, China
Consultant & SAB member (2011.9-) Henry/Chaton Medical Technology Co. Ltd.
Shanghai, China
Consultant & VP of Chemistry (2009.9-) Viva Biotech, Inc.
Zhang Jiang Hi-Tech Park, Shanghai, China
Venture Partner (2008.1-) ePlanet Venture, Global Venture Capital
San Jose, California

American Association of Pharmaceutical Scientists (2000-)
IUPAC (1999-)
American Chemical Society (1994-)
American Association for the Advancement of Science (1993-)
Chinese American Chemical Society (1997-)
Chinese Chemical Society (1987-)
Chinese Nuclear Society (1987-)
Selected Peer-reviewed Publications
1. (new)
2. M. Tavallaie, R. Voshtani, X. Deng, Y. Qiao, F. Jiang, J. P. Collman, L. Fu, “Moderation of Mitochondrial Respiration Mitigates Metabolic Syndrome of Aging” Proceedings of the National Academy of Sciences of the United States of America (PNAS), (4)(2020)ASAP
3. S.W. Lei; D.D. Zhang; Y.Y. Qi; S.R. Chowdhury; R. Sun; J.T. Wang; Y. Du; L. Fu; F.Q. Jiang, “Synthesis and Biological Evaluation of Geniposide derivatives as potent and selective PTPlB inhibitors” European Journal of Medicinal Chemistry, 2020, Accepted.
4. X.X. Deng, M.S. Tavallaie, R. Sun, J.T. Wang, Q.Q. Cai, J. Shen, S.W. Lei, L. Fu, F.Q. Jiang, “Drug Discovery Approaches Targeting the Incretin Pathway” Bioorganic Chemistry 99(2020)103810
5. Y.X. Qiao, C. Dsouza, A.A. Matthews, Y. Jin, W. He, J. Bao, F.Q. Jiang, R. Chandna, R.W. Ge, L. Fu, “Discovery of small molecules targeting GRP78 for antiangiogenic and anticancer therapy” European Journal of Medicinal Chemistry, 193(2020)112228
6. Y. Tian, J. Lin, F. Chen, S. Wang, D. Li, Z. Kuang, W. Zhu, Y. Li, T. Zheng, W. Cao, B. Zhu, E. Tsai, L. Fu, M. Li, “Structure elucidation and formation mechanistic study of a methylene-bridged pregabalin dimeric degradant in pregabalin extended-release tablets” International Journal of Pharmaceutics 575(2020)118910
7. Y. Tian, H.R. Zhang, Z. Zhu, L Chen, E. Wang, J. Jin, D. Li, W. Zhu, M. Li, L. Fu, “A variation of Favorskii rearrangement mechanism under weakly acidic conditions: the case of clobetasol propionate degradation in solution” ChemRxiv, 2020
8. Di Wang, Yafei Liu, Wei Zhu, Hong Shen, Haixia Liu, Lei Fu, “Efficient Synthesis of Substituted Morpholine Derivatives via an Indium (III)-Catalyzed Reductive Etherification Reaction” Chemistry Letters, 49(2020)ASAP, https://doi.org/10.1246/cl.200142
9. Y.X. Qiao, K. Maiti, Z. Sultana, L. Fu, R. Smith, “Inhibition of vertebrate aldehyde oxidase as a therapeutic treatment for cancer, obesity, aging and amyotrophic lateral sclerosis” European Journal of Medicinal Chemistry, 187(2019)111948
10. S.R. Chowdhury, F.Z. Xie, J.X. Gu and L. Fu, “Small-Molecule Amyloid Beta-Aggregation Inhibitors in Alzheimer’s Disease Drug Development” Pharmaceutical Fronts, 1(1)(2019)e22-e32
11. Y. Qiu, M. Lin, G. Chen, C. Fan, M. Li, X. Gu, S. C. Z. Zhao, L. Fu, X. Fang, and Z. Xiao, “Photodegradable CuS SERS Probes for Intraoperative Residual Tumor Detection, Ablation, and Self-Clearance” ACS Applied Material Interfaces, 11(2019)23436-23444
12. M. Kawaguchi-Suzuki, M.G. Law, J. Prisco, K. Head, L. Fu, T. Yumoto, J. Kamei, M. Yang, K. Cheng, M.D. Hogue, “Cultural Sensitivity and Global Pharmacy Engagement in Asia: China, Japan, South Korea, and Taiwan” American Journal of Pharmaceutical Education, 83(4)(2019)Article 7214.
13. F.Z. Xie, Y.Y. Liang, Y. Xia, S.H. Luo, F.Q. Jiang, L. Fu, “Discovery of 2-ethoxy-4-(methoxymethyl) benzamide derivatives as potent and selective PTP1B inhibitors” Bioorganic Chemistry 92(2019)103273
14. L. Li, M.S. Tavallaie, F.Z. Xie, Y. Xia, Y.Y. Liang, F.Q. Jiang, L. Fu, “Identification of lipid-like salicylic acid-based derivatives as potent and membrane-permeable PTP1B inhibitors” Bioorganic Chemistry 93(2019)103296
15. F.Z. Xie, F.Z. Yang, Y.Y. Liang, L. Li, Y. Xia, F.Q. Jiang, W.L. Liu, Y.Y. Qi, S.R. Chowdhury, D.S. Xie, L. Fu, “Investigation of Stereoisomeric Bisarylethenesulfonic Acid Esters for Discovering Potent and Selective PTP1B Inhibitors” European Journal of Medicinal Chemistry, 164(2019)408-422(cited 5)
16. R. Sun, X.X. Deng, D. Zhang, F.Z. Xie, D. Wang, J. Wang, M.S. Tavallaie, F.Q. Jiang, L. Fu, “Anti-diabetic Potential of Pueraria Lobata Root Extract Through Promoting Insulin Signaling by PTP1B Inhibition” Bioorganic Chemistry, 87(2019)12-15


17. X. Deng, J. Shen, H. Zhu, J. Xiao, R. Sun, F. Xie, C. Lam, J. Wang, Y. Qiao, M. Tavallaie, Y. Hu, J. Li, L. Fu, F.Q. Jiang, “Surrogating and redirection of pyrazolo[1,5-a]pyrimidin-7(4H)-one core, a novel class of potent and selective DPP-4 inhibitors” Bioorganic & Medicinal Chemistry, 26(2018)903-912
18. W. Zhang, J.B. Liu, J.M. Macho, X.Z. Jiang, D.S. Xie, F.Q. Jiang, W.L. Liu, L. Fu, “Design, synthesis and antimicrobial evaluation of novel benzoxazole derivatives” European Journal of Medicinal Chemistry, 126(2017)7-14
19. Wan He, Yong Zhang, Jian Bao, Xinxian Deng, Jennifer Batara, Shawn Casey, Qiuyuan Guo, Faqin Jiang, Lei Fu, “Synthesis, biological evaluation and molecular docking analysis of 2-phenyl-benzofuran-3-carboxamide derivatives as potential inhibitors of Staphylococcus aureus Sortase A” Bioorganic & Medicinal Chemistry, 25(2017)1342-1351
20. Jin Xie, Fengzhi Yang, Man Zhang, Celine Lam, Yixue Qiao, Jia Xiao, Dongdong Zhang, Yuxuan Ge, Lei Fu, Dongsheng Xie, “Antiproliferative activity and SARs of caffeic acid esters with mono-substituted phenylethanols moiety” Bioorganic & Medicinal Chemistry Letters, 27(2017)131-134
21. Fengzhi Yang, Fangzhou Xie, Ying Zhang, Yu Xia, Wenlu Liu, Faqin Jiang, Celine Lam, Yixue Qiao, Dongsheng Xie, Jianqi Li, Lei Fu, “Y-shaped bis-arylethenesulfonic acid esters: Potential potent and membrane permeable protein tyrosine phosphatase 1B inhibitors” Bioorganic & Medicinal Chemistry Letters, 27(2017)2166-2170
22. D.S. Xie, J. Lu, J. Xie, J.J. Cui, T.F. Li, Y.C. Wang, Y. Chen, N. Gong, X.Y. Li, L. Fu, Y.X. Wang, “Discovery and analgesic evaluation of 8-chloro-1,4-dihydropyrido[2,3-ß]pyrazine-2,3-dione as a novel potent D-amino acid oxidase inhibitor” European Journal of Medicinal Chemistry, 117(2016)19-32
23. X.W. Chen, Y.Y. Sun, L. Fu, J.Q. Li, “Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl) amides as potential multireceptor atypical antipsychotics” European Journal of Medicinal Chemistry, 123(2016)332-353
24. Y. Zhang, J. Bao, X.X. Deng, W. He, J.J. Fan, F.Q. Jiang, L. Fu, “Synthesis, biological evaluation and molecular docking of 2-phenyl-benzo[d]oxazole-7-carboxamide derivatives as potential Staphylococcus aureus Sortase A inhibitors” Bioorganic & Medicinal Chemistry Letter., 26(16)(2016)4081-4085
25. W. He, B.Z. Xu, J. Bao, X.X. Deng, W.L. Liu, Y. Zhang, F.Q. Jiang, L. Fu, “Synthesis and antimicrobial evaluation of 3-substituted-imine-6-hydroxy-benzofuran derivatives” Med. Chem. Res., 25(11)(2016) 2485-2497
26. Y. Jin, X.H. Cheng, F.Q. Jiang, Z. Guo, J. Xie, L. Fu, “Application of the ultrafiltration-based LC-MS approach for screening PTP1B inhibitors from Chinese red yeast rice” Analytical Methods, 8(2)(2016)353-361
27. X.W. Chen, F. Ni, Y. Liu, L. Fu, J.Q. Li, “A New and Practical Synthesis of Cariprazine through the Facile Construction of 2-[trans-4-(3,3- Dimethylureido)cyclohexyl]acetic Acid” Synthesis, 48(18)(2016)3120-3126
28. W. Jia, L.Z. Zhao, H.X. Wei, L.D. Zhu, L. Fu, W.C. Chen, “Iron-catalyzed cross-coupling of secondary alkyl chloride and alkynes Grignard reagent” Youji Huaxue, 36(5)(2016)1060-1064
29. X.W. Chen, Y. Liu, X.Q. Jin, Y.Y. Sun, S.L. Gu, L. Fu, J.Q. Li, “Development and Kilogram-Scale Synthesis of a D2/5-HT2A Receptor Dual Antagonist (±)-SIPI 6360” Organic Process Research & Development, 20(9)(2016)1662-1667
30. Y. Jin, X.H. Cheng, F.Z. Yang, L. Fu, “Ultracentrifugation-based multi-target affinity selection mass spectrometry” RSC Advances, 5(130)(2015)107616-107622
31. G.S. Zhou, L. Fu, X.B. Li, “Optimisation of ultrasound-assisted extraction conditions for maximal recovery of active monacolins and removal of toxic citrinin from red yeast rice by a full factorial design coupled with response surface methodology” Food Chemistry, 170(2015)186-192
32. X.X. Deng, J.B. Liu, Y. Jin, Y. Zhang, W. He, J. Bao, W.L. Liu, F.Q. Jiang, L. Fu, “Identification of 2-substituted ethenesulfonic acid ester derivatives as novel, potent and selective inhibitors of protein tyrosine phosphatase 1B” Pharmazie, 70(12)(2015)777-783
33. J.B. Liu, X.X. Deng, Y. Jin, B.Z. Xu, W.L. Liu, F.Q. Jiang, L. Fu, “Design, synthesis, and biological evaluation of 2-substituted ethenesulfonic acid ester derivatives as selective PTP1B inhibitors” Pharmazie, 70(7)(2015)446-451
34. Y.F. Wang, Y. Xia, W.L. Liu, F.Q. Jiang, L. Fu, “Synthetic method of caffeic acid phenethyl ester by Heck reaction” Xiandai Shengwuyixue Jinzhan, 15(1)(2015)9-13
35. F.Z. Yang, M. Zhang, J. Xie, D.S. Xie, L. Fu, “Design, synthesis and antitumor research of aza-peptide michael acceptors” Gaodeng Xuexiao Huaxue Xuebao, 36(5)(2015)914-918
36. D.S. Xie, Y.C. Wang, J. Xie, J. Lu, J.J. Cui, M. Zhang, L. Fu, Y.X. Wang, “Quinoxaline-2,3-diones: potential D-amino acid oxidase (DAAO) inhibitors” Med. Chem. Res., 23(2014)4977-89
37. D.S. Xie, F.Z. Yang, J. Xie, M. Zhang, W.L. Liu, L. Fu, “A rapid and practical catalytic esterification for the preparation of caffeic acid esters” J. of Chem. Res., 38(2014)695-700
38. B.Z. Xu, Z.L. Zhang, L. Fu, “A facile synthesis of novel tricyclic 4-pyridones” Tetrahedron Letters, 55(2014)7194-7
39. L. Zhang, X. Xie, Z. Peng, L. Fu, Z. Zhang, “Ru-catalyzed 1,4-addition of arylboronic acids to acrylic acid derivatives in the presence of phenols” Chem. Commun., 49(78)(2013)8797-9
40. L. Zhang, X. Xie, L. Fu, Z. Zhang, “[RuCl2(p-cymene)]2-catalyzed conjugate addition of arylboronic acids to α,β-unsaturated ketones under ligand-free and neutral conditions” Journal of Organic Chemistry, 78(7)(2013)3434-7
41. F. Ma, X. Xie, L. Zhang, Z. Peng, L. Ding, L. Fu, Z. Zhang, “Palladium-catalyzed amidation of aryl halides using 2-dialkylphosphino-2’-alkoxyl-1,1’-binaphthyl as ligands” Journal of Organic Chemistry, 77(12)(2012)5270-85
42. J.B. Liu, F.Q. Jiang, Y. Jin, Y. Zhang, J.J. Liu, W.L. Liu, L. Fu, “Design, synthesis, and evaluation of 2-substituted ethenesulfonic acid ester derivatives as protein tyrosine phosphatase 1B inhibitors” European Journal of Medicinal Chemistry, 57(2012)10-20
43. J.B. Liu, F.Q. Jiang, X.Z. Jiang, W. Zhang, J.J. Liu, W.L. Liu, L. Fu, “Synthesis and antimicrobial evaluation of 3-methanone-6-substituted-benzofuran derivatives” European Journal of Medicinal Chemistry, 54(2012)879-886
44. W. Zhang, W.L. Liu, X.Z. Jiang, F.Q. Jiang, L. Fu, “One-pot synthesis of hydroxybenzo[d] oxazol-2-aliphatic acid derivatives by the Meerwein’s reagent” Syn. Commun., 42(18)(2012)2772-2779
45. J.J. Liu, X.H. Cheng, L. Fu, “LC-MS based assay method for DPP-IV inhibitor screening and substrate Discovery” Analytical Methods, 4(2012)1797-1805
46. W. Zhang, W.L. Liu, X.Z. Jiang, F.Q. Jiang, H. Zhuang, L. Fu, “Design, synthesis and antimicrobial activity of chiral 2-(substituted-hydroxyl)-3-(benzo[d]oxazol-5-yl)propanoic acid derivatives” European Journal of Medicinal Chemistry, 46(2011)3639-3650
47. X.Z. Jiang, W.L. Liu, W. Zhang, F.Q. Jiang, Z. Gao, L. Fu, “Synthesis and antimicrobial evaluation of new benzofuran derivatives” European Journal of Medicinal Chemistry, 46(2011)3526-3530
48. Z. Gao, X.Z. Jiang, W. Zhang, W.L. Liu, L. Fu, “Synthesis of Water-soluble Resveratrol Analogues” Chinese Journal of New Drugs, 19(2010)748-750.
49. W.L. Liu, J.C. Zhang, F.Q. Jiang, L. Fu, “Synthesis and Cytotoxicity Studies of New Cryptophycin Analogues” Arch. Pharm. Chem. Life Sci., 342(2009)577-583.
50. Y. Chen, Y.D. Peng, J.C. Zhang, L. Fu, “Synthesis and Biological Evaluation of Novel Selenonucleosides” Nucleosides, Nucleotides and Nucleic Acids, 27(2008)1001-1008.
51. N. Lu, Y.D. Peng, J.C. Zhang, L. Fu, “Synthesis of Cidofovir” Chinese Journal of New Drugs, 16(2007)1272-1274.
52. W.H. Wei, Z. Wang, T. Mizuno, C. Cortez, L. Fu, M. Sirisawad, L. Naumovski, D. Magda, J.L. Sessler, “New polyethyleneglycol-functionalized texaphyrins: Synthesis and in vitro biological studies” J. Chem. Soc., Dalton Transactions, 2006, 1934-1942.
53. J. P. Collman, R. Boulatov, C. Soundland and L. Fu, “Functional Analogs of Cytochrome c Oxidase, Hemoglobin and Myoglobin” Chemical Reviews, 104(2004)561-88.
54. T. D. Mody, L. Fu, and J. Sessler, “Texaphyrins: Synthesis and Development of A Novel Class of Therapeutic Agents” Progress in Inorganic Chemistry, 2001, 551-598. (Book Chapter)
55. J. P. Collman and L. Fu, “Synthetic Models for Hemoglobin and Myoglobin” Accounts of Chemical Research, 32(1999)455-463
56. J. P. Collman, L. Fu, P. C. Herrmann, Z. Wang, M. Rapta, M. Broring, R. Schwenninger and B. Boitrel, “A Functional Model of Cytochrome c Oxidase — Thermodynamic Implication” Angew. Chem. International Edition, 37(1998)3397-3400
57. J. P. Collman, L. Fu, P. C. Herrmann, and X. Zhang, “A Functional Model Related to Cytochrome c Oxidase and Its Electrocatalytic Four-Electron Reduction of Dioxygen” Science, 275(1997)949-951


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