傅磊 教授

电话：(86)-
邮箱：leifu@sjtu.edu.cn
主页：fulab.net..cn 上海市闵行区东川路800号生物药学楼7号楼-500


个人简历 研究方向 发表论文 科研成果
傅磊，男，毕业于复旦大学，1984年获化学学士学位、1987年获放射化学专业硕士学位。留校任教三年后，于1990年赴德国柏林自由大学化学系核化学与放射化学研究所参与完成欧共体的大型核燃料工程项目。1993年进入美国斯坦福大学化学系，师从James P. Collman教授，开展对血色素、肌球素和线粒体中细胞色素c氧化酶的结构和功能研究。于1997年初获得斯坦福大学博士学位。毕业后曾在斯坦福大学继续一年多的博士后工作，于1998年加入美国Pharmacyclics公司（已被AbbVie公司收购），从事于新型抗肿瘤和心血管疾病核磁成像诊断和化学药物的临床前研究，主要负责药物的设计、合成和优化，药物活性的研究，药物生产工艺的设计、优化，以及药物代谢过程的研究，这些药物已经进入不同阶段的临床试验。
傅磊博士于2007年初正式受聘于上海交通大学药学院，任药物化学专业课题组组长。课题组的科学研究涉及到化学新药的设计、合成及其抗肿瘤、糖尿病、心血管疾病和慢性疼痛等方面的临床前研究；药物生产工艺及药品中有关物质的研究；线粒体活性调控机制及临床应用探索。为本科生、研究生开设了《药物化学原理》、《科学表达实践》、《Comprehensive Pharmacy》、《药学、化学山海经》、《管理生命的智慧》、《药学专业前沿》等英语或双语课程，自2011年交大开展评教以来，开设的新生研讨评教结果蝉联药学院、学校前茅。
傅磊教授主持、参与过包括上海市教委、外交部、国家自然基金以及与国内外高校和药企合作等科研合作项目，至今已获得专利授权20多个，在学术权威杂志上发表论文70多篇，例如《科学》、《PNAS》、《化学综述》、《化学研究前沿》、《美国化学会杂志》、《德国应用化学》以及《有机化学杂志》等。担任《Bioorganic Chemistry》期刊的副主编、《中国医药工业杂志》及其英文版《Pharmaceutical Fronts》的编委、上海市药学会药物化学委员会委员、中国医药生物技术协会生物医药信息分会副主任委员、中国非公立医疗机构协会物联网医疗专业委员会常务委员等。
傅磊教授还与埃塞尔比亚 亚的斯亚贝巴大学的世界银行CDT卓越中心合作，多次赴非洲，主持研究非洲传统植物药，指导当地研究生的科研工作，在世界银行的帮助下创建非洲药典。获得了中国外交部《发掘非洲传统医药资源，推进中非卫生防疫合作》项目的资助。

课题组的科学研究涉及到化学新药的设计、合成及其抗肿瘤、糖尿病、心血管疾病和慢性疼痛等方面的临床前研究；药物生产工艺及药品中有关物质的研究；线粒体活性调控机制及临床应用探索。

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2020:
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
https://doi.org/10.1073/pnas.
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
2019:
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
2018:
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
2017:
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
2016:
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-?]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
2015:
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
2014:
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
2013:
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
2012:
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
2011:
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
2010-:
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



1) Liu, JB; Jiang, FQ; Jin, Y; Zhang, Y; Liu, JJ Liu, WL; Fu, L; Design, synthesis, and evaluation of 2-substituted ethenesulfonic acid ester derivatives as protein tyrosine phosphatase 1B inhibitors European Journal of Medicinal Chemistry 2012, 57:10-20
2) Liu, JB; Jiang, FQ; Jiang, XZ; Zhang, W; Liu, JJ; Liu, WL; Fu, L; Synthesis and antimicrobial evaluation of 3-methanone-6-substituted-benzofuran derivatives European Journal of Medicinal Chemistry, 2012, 54,879-886
3) Ma, FF; Xie, XM; Zhang, L; Peng, ZY; Ding, LN; Fu, L and Zhang, ZG; Palladium-Catalyzed Amidation of Aryl Halides Using 2-Dialkylphosphino-2′-alkoxyl-1,1′-binaphthyl as Ligands. The Journal of Organic Chemistry, 2012,77(12):5279-5285
4) Zhang, W; Liu, WL; Jiang, XZ; Jiang, FQ; Fu, L; One-pot synthesis of hydroxybenzo[d]oxazole-2-aliphatic acid deribatives by the Meerwein’s reagent. Synthetic Communication, 2012, 42: 2772-2779
5) Liu, JJ; Cheng, XH; Fu, L; LC-MS based assay method for DPP-IV inhibitor screening and substrate discovery. Analytical Methods, 2012, 4:1797-1805
6) Zhang, W; Liu, WL; Jiang, XZ; Jiang, FQ; Zhuang, H; Fu, L; Design, synthesis and antimicrobial activity of chiral 2-(substituted-hydroxyl)- 3-(benzo[d]oxazol-5-yl)propanoic acid derivatives. European Journal of Medicinal Chemistry, 2011, 46, 3639 - 3650
7) Jiang, XZ; Liu, WL; Zhang, W; Jiang, FQ; Fu L; Synthesis and antimicrobial evaluation of new benzofuran derivatives. European Journal of Medicinal Chemistry, 2011, 46, 3526-3530
8) Liu, WL; Jiang, FQ; Liu, JB; Zhang, JC; Fu, L; Synthesis of bis-ANS fluorescence probe in ionic liquids. Chinese Chemical Letters, 2009, 20, 645–647
9) Liu, WL; Zhang, JC; Jiang, FQ; Fu, L; Synthesis and Cytotoxicity Studies of New Cryptophycin Analogues. Arch. Pharm. Chem. Life Sci, 2009, 342, 577 – 583
10) Chen, Y; Peng, YD; Zhang, JC; Fu, L; Synthesis and biological evaluation of novel selenonucleosides. Nucleosides, Nucleotides and Nucleic Acids, 2008, 27, 1001-1008