Lei Fu

Profile

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 then 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 2006. The research in his group interfaces chemistry and medicine. His principal interests are 1) drug discovery and development; 2) process research on drug APIs 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 American Chemical Society, Accounts of Chemical Research, 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.
  • Qualifications

    • 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)
  • Experience

    • Associate Dean for Learning and Teaching(2020.12 to present)Academy of Pharmacy, XJTLU
    • Professor of Medicinal Chemistry (2006.3-2020.11) 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
  • Research interests

    • Human Hibernation Studies using Biomimetic Models of Cytochrome c Oxidase.
    • Medical Devices as Targeted Drug Delivery Systems
    • Traditional Chinese Medicines as Botanical Cosmeceuticals
    • Process Research on Drug APIs and Related Substances
    • Drug Discovery and Development for Metabolic and Neurodegenerative Diseases
  • Articles

    • Luo S, Dang X, Wang J, Yuan C, Hu Y, Lei S, Zhang Y, Lu D, Jiang F, Fu L. Biological evaluation of mitochondria targeting small molecules as potent anticancer drugs. Bioorg Chem. 2021 Jun 3;114:105055. doi: 10.1016/j.bioorg.2021.105055. Epub ahead of print. PMID: 34144278.
    • Dang X, Lei S, Luo S, Hu Y, Wang J, Zhang D, Lu D, Jiang F, Fu L. Design, synthesis and biological evaluation of novel thiazole-derivatives as mitochondrial targeting inhibitors of cancer cells. Bioorg Chem. 2021 May 25;114:105015. doi: 10.1016/j.bioorg.2021.105015. Epub ahead of print. PMID: 34139611.
    • Chowdhury SR, Gu J, Hu Y, Wang J, Lei S, Tavallaie MS, Lam C, Lu D, Jiang F, Fu L. Synthesis, biological evaluation and molecular modeling of benzofuran piperidine derivatives as Aβ antiaggregant. Eur J Med Chem. 2021 May 25;222:113541. doi: 10.1016/j.ejmech.2021.113541. Epub ahead of print. PMID: 34116326.
    • J. Shen, X. Deng, R. Sun, M.S. Tavallaie, J. Wang, Q. Cai, C. Lam, S. Lei, L. Fu, F. Jiang, Structural optimization of pyrazolo[1,5-a]pyrimidine derivatives as potent and highly selective DPP-4 inhibitors, European Journal of Medicinal Chemistry, https://doi.org/10.1016/ j.ejmech.2020.112850.
    • 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), (117)(2020)(18)9840-9850, https://doi.org/10.1073/pnas.1917948117
    • 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.
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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.
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • B.Z. Xu, Z.L. Zhang, L. Fu, “A facile synthesis of novel tricyclic 4-pyridones” Tetrahedron Letters, 55(2014)7194-7
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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.
    • 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.
    • 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.
    • N. Lu, Y.D. Peng, J.C. Zhang, L. Fu, “Synthesis of Cidofovir” Chinese Journal of New Drugs, 16(2007)1272-1274.
    • 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.
    • 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.
    • 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)
    • J. P. Collman and L. Fu, “Synthetic Models for Hemoglobin and Myoglobin” Accounts of Chemical Research, 32(1999)455-463
    • 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
    • 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
  • Professional service activities

    • Adjunct Professor (2015.03-present) Roosevelt University College of Pharmacy, Schaumburg, IL 60173, USA
    • Adjunct Professor (2013.05-present) Santa Clara University School of Engineering, Bioengineering Department ,Santa Clara, California, USA
    • Visiting Professor (Summers of 2009, 2010 & 2016-present) Stanford University Department of Chemistry Stanford, California, USA
    • Consultant & SAB member (2013.9-present) Blue Bay Science & Technology Co. Ltd. Xiamen, China
    • Consultant & SAB member (2011.9-present) Henry/Chaton Medical Technology Co. Ltd. Shanghai, China
    • Consultant & VP of Chemistry (2009.9-present) Viva Biotech, Inc. Zhang Jiang Hi-Tech Park, Shanghai, China
    • Venture Partner (2008.1-present) ePlanet Venture, Global Venture Capital San Jose, California
  • Professional memberships

    • American Association of Pharmaceutical Scientists (2000-present)
    • IUPAC (1999-present)
    • American Chemical Society (1994-present)
    • American Association for the Advancement of Science (1993-present)
    • Chinese American Chemical Society (1997-present)
    • Chinese Chemical Society (1987-present)
    • Chinese Nuclear Society (1987-present)
  • 电话

    +86 (0)512 88973019
  • 电子邮件

    Lei.Fu@xjtlu.edu.cn
  • 地址

    SD334F (Science Building)
    Suzhou Dushu Lake Science and Education Innovation District
    Suzhou Industrial Park
    Suzhou
    P.R.China
    215123