Xiaoguang Lei,Ph.d 

      Department of Chemical Biology
      College of Chemistry and Molecular Engineering,  Peking University,
      Beijing 100871, P. R. China

     Room A509, 
     College of Chemistry and Molecular Engineering,
     Peking University, Beijing, 100871, China

     Tel: +86-10-6276-0292



2001 – 2006    Ph.D. in Organic Synthesis and Chemical Biology       Boston University, Boston, USA

Advisor:  Professor John A. Porco, Jr.

Thesis: “Target and Diversity-Oriented Synthesis Using Epoxyquinoid Scaffolds”

1997 – 2001 B.S. in Chemistry      Peking University, Beijing, China

Advisor:  Professor Jianbo Wang


Professional Experience

2014 – Current    Professor, Department of Chemical Biology, College of Chemistry and Molecular Engineering, Peking University, China

2008 – 2014    Principal Investigator and Director of Chemistry Center, National Institute of Biological Sciences (NIBS), Beijing, China

2010 – 2013     Professor, College of Pharmaceutical Science and Technology, Tianjin University

2008 – 2010     Associate Professor, College of Pharmaceutical Science and Technology, Tianjin University, China

2006 – 2008    Post-doctoral Fellow, Bioorganic Chemistry, Columbia University and Memorial Sloan-Kettering Cancer Center, New York, NY, USA     

Advisor: Professor Samuel J. Danishefsky


Honors and Awards

  • David Ginsburg Memorial Lectureship Award, 2018
  • CCS-BASF Young Investigator Award, 2018
  • Tetrahedron Young Investigator Award in Bioorganic and Medicinal Chemistry, 2017
  • Swiss Chemical Society Distinguished Lectureship Award, 2017
  • KAIST School of Molecular Science Lectureship Award, 2017
  • Asian Core Program Lectureship Award, 2016
  • Organic Chemistry Frontier Emerging Investigator Award, 2016
  • National Distinguished Young Investigator Award, 2016
  • Wei Shan Natural Product Synthesis Award by Chinese Chemical Society, 2015
  • Chemical Society of Japan Distinguished Lectureship Award, 2015
  • Outstanding Young Talent Award of Beijing, 2014
  • Roche Chinese Young Investigator Award, 2014
  • National Leading Young Scientific Investigator Award, 2013
  • Chinese Chemical Society Prize for Young Scientists, 2013
  • Young Chemical Biologist Award by the International Chemical Biology Society (ICBS), 2013
  • Servier Young Investigator Award by Chinese Pharmaceutical Association, 2013
  • Thieme Chemistry Journal Award, 2013
  • Asian Core Program Lectureship Award, 2012
  • Outstanding Young Investigator Award by National Natural Science Foundation of China, 2012
  • New Century Excellent Talents in University Award, 2010
  • WuXi PharmaTech 2010 Life Science and Chemistry Award, 2010
  • IUPAC Young Chemist Award, 2009
  • NESACS-JCF/GDCh Exchange Scholarship to Germany, 2005
  • Travel Award for the Gordon Research Conference on Combinatorial Chemistry, 2005
  • Sugata Ray Memorial Award for Excellence in Research and Teaching at Boston University,  2005



  • Member, International Chemical Biology Society (ICBS)
  • Member, Chinese-American Chemistry Professor Association (CAPA)
  • Member, American Chemical Society
  • Member, Chinese Chemical Society
  • Member, Chinese Pharmaceutical Association


Professional Service

Editor, Bioorganic and Medicinal Chemistry, 2017

Editorial Board Member, Bioorganic and Medicinal Chemistry (Letters), 2016-

Editorial Board Member, Advanced Science, 2015-

Editorial Board Member, Natural Product Research and Development, 2015-

Manuscript Referee

Nature Chemical Biology (March 2013–Present)

Nature Cell Biology (April 2014–Present)

Nature Communication (October 2013–Present)

Cell Chemical Biology (September 2015–Present)

Angewandte Chemie, International Edition (July 2008–Present)

Chemical Communications (August 2008–Present)

Chemistry: A European Journal (December 2008–Present)

Chemistry: An Asian Journal (March 2009–Present)

European Journal of Organic Chemistry (November 2008–Present)

Organic and Biomolecular Chemistry (January 2010–Present)

Organic Letters (October 2008–Present)

Journal of the American Chemistry Society (August 2011–Present)

Journal of Organic Chemistry (January 2010–Present)


Research Interests

  • Chemical biology
  • Natural product total synthesis
  • Medicinal chemistry



  1. Dong Q, Li X, Wang CZ, Xu S, Yuan G, Shao W, Liu B, Zheng Y, Wang H, Lei X, Zhang Z, Zhu B.* “Roles of the CSE1L-mediated nuclear import pathway in epigenetic silencingProc Natl Acad Sci U S A. 2018, doi: 10.1073/pnas.1800505115
  2. Ozaki T, Shinde SS, Gao L, Okuizumi R, Liu C, Ogasawara Y, Lei X, Dairi T, Minami A, Oikawa H.* “Enzymatic formation of a skipped methyl-substituted octaprenyl side chain of longestin (KS-505a): Involvement of homo-IPP as a common extender unit” Angew. Chem. Int. Ed. 2018, doi: 10.1002/anie.201802116
  3. Li X, Shang E, Dong Q, Li Y, Zhang J, Xu S, Zhao Z, Shao W, Lv C, Zheng Y, Wang H, Lei X, Zhu B,* Zhang Z.* “Small molecules capable of activating DNA methylation-repressed genes targeted by the p38 mitogen-activated protein kinase pathway” J. Biol. Chem. 2018, doi: 10.1074/jbc.RA117.000757.
  4. Gubu, A.; Li, L.; Ning, Y.; Zhang, X.; Lee, S.; Feng, M.; Li, Q.; Lei, X.; Jo, K.; Tang, X.* “Bioorthogonal Metabolic DNA Labelling using Vinyl Thioether-Modified Thymidine and o-Quinolinone Quinone Methide” Chem. Eur. J. 2018, 24, 5895-5900
  5. Yue, Z.; Xiao, X.; Wu, J.; Zhou, X.; Liu, W.; Liu, Y.; Li, H.; Chen, G.; Wu, Y.*; Lei, X.*ent-Jungermannenone C Triggers Reactive Oxygen Species-Dependent Cell Differentiation in Leukemia Cells” J. Nat. Prod. 2018, 81, 298-306
  6. Zhang, X.; Wang, J.; Tan, D.; Li, Q.; Li, M.; Gong, Z.; Tang, C.; Liu, Z.; Dong, W.*; Lei, X.* “Carboxylate-Selective Chemical Cross-Linkers for Mass Spectrometric Analysis of Protein Structures” Anal. Chem. 2018, 90, 1195-1201
  7. Li, H.; Lei, X.*Fawcettimine-Type Lycopodium Alkaloids as a Driving Force for Discoveries in Organic SynthesisChem. Rec. 2017 Dec 18. doi: 10.1002/tcr.201700047
  8. Narita, K.; Sato, H.; Minami, A.; Kudo, K.; Gao, L.; Liu, C.; Ozaki, T.; Kodama, M.; Lei, X.; Taniguchi, T.; Monde, K.; Yamazaki, M.; Uchiyama, M.; Oikawa, H.* “Focused Genome Mining of Structurally Related Sesterterpenes: Enzymatic Formation of Enantiomeric and Diastereomeric ProductsOrg. Lett. 2017, 19, 6696-6699.
  9. Zhang, J.; Wang, S.; Bai, Y.; Guo, Q.; Zhou, J.; Lei, X.* “Total Syntheses of Natural Metallophores Staphylopine and Aspergillomarasmine A” J. Org. Chem. 2017, 82, 13643-13648.
  10. Zhang, J.; Wang, S.; Wei, Q.; Guo, Q.; Bai, Y.; Yang, S.; Song, F.; Zhang, L.; Lei, X.*Synthesis and biological evaluation of Aspergillomarasmine A derivatives as novel NDM-1 inhibitor to overcome antibiotics resistance.Bioorg. Med. Chem. 2017, 25, 5133-5141.
  11. Han, X.; Yang, Y.; Wu, Y.; Liu, X.; Lei, X.*; Guo, Y.* “A bioassay-guided fractionation system to identify endogenous small molecules that activate plasma membrane H+-ATPase activity in Arabidopsis.” J. Exp. Bot. 2017, 68, 2951-2962.
  12. Hong, B.; Hu, D.; Wu, J.; Zhang, J.; Li, H.; Pan, Y.; Lei, X.* “Divergent Total Syntheses of (-)-Huperzine Q, (+)-Lycopladine B, (+)-Lycopladine C and (-)-epi-Lycopladine D” Chem. Asian J. 2017, 12, 1557-1567. (VIP paper)
  13. Zhuang, S.; Li, Q.; Cai, L.; Wang, C.*; Lei, X.* “Chemoproteomic Profiling of Bile Acid Interacting Proteins” ACS Cent. Sci. 2017, 3, 501-509.
  14. Jones, A.; Zhang, X.; Lei, X.* “Covalent Probe Finds Carboxylic Acid” Cell Chem. Biol. 2017, 24, 537-538.
  15. Ren, Y.; Su, Y.; Su, L.; He, S.; Meng, L.; Liao, D.; Liu, X.; Ma, Y.; Liu, C.; Li, S.; Ruan, H.; Lei, X.; Wang, X.*; Zhang, Z.* “Discovery of a Highly Potent, Selective, and Metabolically Stable Inhibitor of Receptor-Interacting Protein 1 (RIP1) for the Treatment of Systemic Inflammatory Response Syndrome” J. Med. Chem. 2017, 60, 972-986.
  16. Siridechakorn, I.; Yue, Z.; Mittraphab, Y.; Lei, X.Pudhom, K.* “Identification of spirobisnaphthalene derivatives with anti-tumor activities from the endophytic fungus Rhytidhysteron rufulum AS21B” Bioorg. Med. Chem. 2017, 25, 2878-2882.
  17. Liu, X.; Dong, T.; Zhou, Y.; Huang, N.; Lei, X.* “Exploring the Binding Proteins of Glycolipids with Bifunctional Chemical Probes” Angew. Chem. Int. Ed. 2016, 55, 14330-14334.
  18. Tan, D.; Li, Q.; Zhang, M.; Liu, C.; Ma, C.; Zhang, P.; Ding, Y.; Fan, S.; Tao, L.; Yang, B.; Li, X.; Ma, S.; Liu, J.; Feng, B.; Liu, X.; Wang, H.; He, S.; Gao, N.; Ye, K.; Dong, M.*; Lei, X.* “Trifunctional Cross-Linker for Mapping  Protein-Protein Interaction Networks and Comparing  Protein Conformational States” eLife 2016; 5:e12509. (News story describing this work was highlighted by Nature Methods 2016, 13, 392-392).
  19. Li, C.; Jones, A.; Lei, X.* “Synthesis and Mode of Action of Oligomeric Sesquiterpene Lactones” Nat. Prod. Rep. 2016, 33, 602-611. (Cover story)
  20. Shang, E.; Zhang, J.;  Bai, J.; Wang, Z.; Li, X.; Zhu, B.; Lei, X.* “Syntheses of [1,2,4]triazolo[1,5-a]benzazoles Enabled by the Transition-Metal-Free Oxidative N-N Bond Formation”  Chem. Commun. 201652, 7028-7031.
  21. Liao, D.; Yang, S.; Wang, J.; Zhang, J. Hong, B.; Wu, F.; Lei, X.* “Total Synthesis and Structural Reassignment of Aspergillomarasmine A” Angew. Chem. Int. Ed. 2016, 55, 4291-4295.
  22. Liu, W.; Li, H.; Cai, P.; Wang, Z.; Yu, Z-X.; Lei, X.* “Scalable Total Synthesis of Jungermannenones B and C” Angew. Chem. Int. Ed. 2016, 55, 3112-3116. (Highlighted by Synfacts 2016, 12, 0332).
  23. Li, D.; Li, C.; Li, L.; Chen. S.; Wang, L.; Li, Q.; Wang, X.; Lei, X.*; Shen, Z.* “Natural Product Kongensin A is a Non-Canonical HSP90 Inhibitor that Blocks RIP3-dependent Necroptosis” Cell Chem. Biol. 2016, 23, 257-266. (Featured article, and highlighted by Jacobsen et al. Cell Chem. Biol. 2016, 23, 205-207).
  24. Gao, L.; Han, J.; Lei, X.* “Enantioselective Total Syntheses of Kuwanon X, Kuwanon Y and Kuwanol A” Org. Lett. 2016, 18, 360-363.
  25. Yang, S.; Liao, D.; Tian, X.; Lei, X.* “Access to the 2H-tetrahydro-4, 6-dioxo-1, 2-oxazine Ring System from Nitrone via a Tandem Nucleophilic Addition and Transesterification Re-action” Org. Lett. 2016, 18, 376-379.
  26. Dong, T.; Liu, W.; Shen, Z.; Li, L.; Chen, S.; Lei, X.* “Pterisolic Acid B is a Nrf2 Activator by Targeting C171 within Keap1-BTB Domain” Sci. Rep. 2016, 6, 19231.
  27. Ma, K.; Liao, D.; Yang, S.; Li, X.; Lei, X.* “Studies towards the Synthesis of the Functionalized C3-C14 Decalin Framework of Alchivemycin A” Org. Chem. Front. 2016, 3, 251-258.
  28. Li, X.; Han, J.; Jones, A.; Lei, X.* “Chiral Boron Complex-Promoted Asymmetric Diels-Alder Cycloaddition and Its Application in Natural Product Synthesis” J. Org. Chem. 2016, 81, 458-468.
  29. Hong, B.; Li, C.; Wang, Z.; Chen, J.; Li, H.*; Lei, X.* “Enantioselective Total Synthesis of (-)-Incarviatone A” J. Am. Chem. Soc. 2015, 137, 11946-11949. (News story describing this work was highlighted by Chem. & Eng. News 2015, 93, 35 and Synfacts 2015, 11, 1231).
  30. Dong, T.; Liao, D.; Liu, X.; Lei, X.* “Using Small Molecules to Dissect Non-apoptotic Programmed Cell Death” ChemBioChem 2015, 16, 2557-2561.
  31. Ren, R.; Zhou, X.; He, Y.; Ke, M.; Wu, J.; Liu, X.; Yan, C.; Wu, Y.; Gong, X.; Lei, X.; Yan, S. F.; Radhakrishnan, A.; Yan, N.* “Crystal structure of a mycobacterial Insig homolog provides insight into how these sensors monitor sterol levels” Science 2015, 349, 187-191.
  32. Li, T.; Liu, W.; Lu, S.; Zhang, Y-P.; Jia, L-M.; Chen, J.; Li, X.; Lei, X.; Dong, M.* “No Significant Increase in the Δ4- and Δ7-Dafachronic Acid Concentration in the Long-Lived glp-1 Mutant and in Dauer Formation-Defective Mutants” G3: Genes/Genomes/Genetics 2015, DOI: 10.1534/g3.115.018812
  33. Zhang, X.; Dong, T.; Li, Q.; Liu, X.; Li, L.; Chen, S.; Lei, X.* “Second-Generation TQ-Ligation for Cell Organelle Imaging” ACS Chem. Biol. 2015, 10, 1676-1683.
  34. Han, J.; Jones, A.; Lei, X.* “Recent Advances in the Total Synthesis of Prenylflavonoid and Related Diels-Alder Natural ProductsSynthesis 2015, 47, 1519-1533.
  35. Dong, T.; Li, C.; Wang, X.; Dian, L.; Zhang, X.; Chen, X.; Li, L.; Cao, R.; Huang, N.; He, S. *; Lei, X.* Ainsliadimer A selectively inhibits IKKα/β by covalently binding a conserved cysteineNature Commun. 2015, 6, 6522. (News story describing this work was highlighted in Chem. & Eng. News 2015, 15, 39).
  36. Liu, W.; Li, X.; Chen, J.; Li, T.; Dong, M.; Lei, X.* “Site-selective and Metal-free Aliphatic C-H Oxidation Enabled Synthesis of [5,24,25-D3]-(25S)-Δ7-Dafachronic acid” Chem. Eur. J. 2015, 21, 5345-5379
  37. Hong, B.; Li, H.; Wu, J.; Zhang, J. Lei, X.* “Total Syntheses of (-)-Huperzine Q and (+)-Lycopladines B and C” Angew. Chem. Int. Ed. 2015, 54, 1011-1015. (Highlighted by Synfacts 2015, 11, 0112)
  38. Qin, X.; Chen, B.; Fu, J.; Shan, L.; Lei, X.; Zhang, W.* “Synthesis, cytotoxicity and inhibition of NO production of ivangustin enantiomer analogues” Eur. J. Med. Chem. 2015, 102, 256-265.
  39. Zhang, J.; Chen, J.; Zhang, X.; Lei, X.* “Total Syntheses of Menisporphine and Daurioxoisoporphine C Enabled by Photoredox-Catalyzed Direct C–H Arylation of Isoquinoline with Aryldiazonium Salt” J. Org. Chem. 2014, 79, 10682-10688
  40. Li, C.; Dong, T.; Li, Q.; Lei, X.* “Probing the Anti-cancer Mechanism of (-)-Ainsliatrimer A through Diverted Total Synthesis and Bioorthogonal Ligation” Angew. Chem. Int. Ed. 2014, 53, 12111-12115
  41. Zhang, J.; Wu, J.; Hong, B.; Ai, W.; Wang, X.; Li, H.; Lei, X.* “Diversity-oriented synthesis of Lycopodium alkaloids inspired by the hidden functional group pairing pattern” Nature Commun. 2014, 5, 4614
  42. Han, J.; Li, X.; Guan, Y.; Zhao, W.; Wullf, W. D.*; Lei, X.* “Enantioselective Biomimetic Total Syntheses of Kuwanons I and J and Brosimones A and B” Angew. Chem. Int. Ed. 2014, 53, 9257-9261
  43. Li, C.; Lei, X.* “Strategies toward the Biomimetic Syntheses of Oligomeric Sesquiterpenoids”    J. Org. Chem. 2014, 79, 3289-3295
  44. Liao, D.; Sun, L.; Liu, W.; He, S.; Wang, X.; Lei, X.* “Necrosulfonamide Inhibits Necroptosis by Selectively Targeting the Mixed Lineage Kinase Domain-like Protein” Med. Chem. Comm. 2014, 5, 333-337.
  45. Li, Q.; Dong, T.; Liu, X.; Zhang, X.; Yang, X.; Lei, X.*ortho-Quinone Methide Finds Its Application in Bioorthogonal Ligation” Curr. Org. Chem. 2014, 18, 86-92.
  46. Li, T.; Chen, J.; Li, X.; Ding, X.; Wu, Y.; Zhao, L.; Chen, S.; Lei, X.*; Dong, M.* “Absolute Quantification of a Steroid Hormone that Regulates Development in Caenorhabditis elegansAnal. Chem. 2013, 85, 9281-9287.
  47. Wang, X.; Li, H.; Lei, X.* “Challenges and Strategies to the Total Syntheses of Fawcettimine-Type and Serratinine-Type Lycopodium Alkaloids” Synlett. 2013, 241032-1043 (Invited Synpacts Article).
  48. Li, Q.; Dong, T.; Liu, X.; Lei, X.* “A Bioorthogonal Ligation Enabled by Click Cycloaddition of o-Quinolinone Quinone Methide and Vinyl Thioether” J. Am. Chem. Soc. 2013, 135, 4996-4999. (News story describing this work was highlighted in Chem. & Eng. News 2013, 14, 37).
  49. Li, C.; Dong, T.; Dian, L.; Zhang, W.; Lei, X.* “Biomimetic Syntheses and Structural Elucidation of the Apoptosis-Inducing Sesquiterpenoid Trimers: (-)-Ainsliatrimers A and B” Chem. Sci. 2013, 4, 1163-1167.
  50. Wang, G.*; Wang, X.; Yu, H.; Wei, S.; Williams, N.; Holmes, D. L.; Halfmann, R.; Naidoo, J.; Wang, L.; Li, L.; Chen, S.; Harran, P.; Lei, X.*; Wang, X.* “Small Molecule Activation of the TRAIL Receptor DR5 in Human Cancer Cells” Nature Chem. Biol. 2013, 9, 84-89. (News stories describing this work were highlighted in Chem. & Eng. News 2013, 2, 37; Nature Asia 2012, December 24).
  51. Huang, J.; Lei, X.* “A Nature-inspired Concise Synthesis of (+)-ent-Chromazonarol” Sci. China Chem. 2013, 56, 349-353.
  52. Li, H.; Wang, X.; Hong, B.; Lei, X.* Collective Synthesis of Lycopodium Alkaloids and Tautomer Locking Strategy for the Total Synthesis of (-)-Lycojapodine AJ. Org. Chem. 2013, 78, 800-821. (Featured and Cover Article).
  53. Li, C.; Li, X.; Wang, X.; Lei, X.* “Diversity-Oriented Synthesis of Bicyclic Ring Systems via a Conjugate Addition/Aldol/RCM Process” Sci. China Chem. 2013, 56, 337-341.
  54. Li, C.; Dian, L.; Zhang, W.; Lei, X.* “Biomimetic Syntheses of (-)-Gochnatiolides A-C and (-)-Ainsliadimer B” J. Am. Chem. Soc. 2012, 134, 12414-12417.
  55. Lei, X.*; Li, H. “Selective Alkene Metathesis in the Total Synthesis of Complex Natural Product” Top. Curr. Chem. 2012, 327, 163-196.
  56. Sun, L.; Wang, H.; Wang, Z.; He, S.; Chen, S.; Liao, D.; Wang, L.; Yan, J.; Liu, W.; Lei, X.*; Wang, X.* “Mixed Lineage Kinase Domain-like Protein Mediates Necrosis Signaling Downstream of  RIP3 Kinase” Cell 2012, 148, 213-227. (News stories describing this work were highlighted in Chem. & Eng. News 2012, 5, 40; Nature China 2012, February 1; Asian Scientist 2012, January31; and Nature Reviews Molecular Cell Biology, 2012, Feb. 8).
  57. Li, H.; Wang, X.; Lei, X.* “Total Syntheses of Lycopodium Alkaloids (+)-Fawcettimine, (+)-Fawcettidine and (-)-8-Deoxyserratinine” Angew. Chem. Int. Ed. 2012, 51, 491-495; Angew. Chem. 2012, 124, 506-510.
  58. Liao, D.; Li, H.; Lei, X.* “Efficient Generation of ortho-Quinone Methide: Application to the Biomimetic Syntheses of (±)-Schefflone and Tocopherol Trimers” Org. Lett. 2012, 14, 18-21.
  59. Li, C.; Tu, S.; Wen, S.; Li, S.; Chang, J.; Shao, F.; Lei, X.* “Total Synthesis of the G2/M DNA Damage Checkpoint Inhibitor Psilostachyin C” J. Org. Chem. 2011, 76, 3566-3570.
  60. Li, C.; Yu, X.; Lei, X.* “A Biomimetic Total Synthesis of (+)-Ainsliadimer A” Org. Lett. 2010, 12, 4284-4287.
  61. Gong, Y.; Wang, X.; Wang, J.; Yang, Z.; Li, S.; Yang, J.; Liu, L.; Lei, X.*; Shao, F. * “Chemical Probing Reveals Insights into the Signaling Mechanism of Inflammasome Activation” Cell Res. 2010, 20, 1289-1305.
  62. HanZ.; Niu, T.; Chang, J.; Lei, X.; Zhao, M.; Wang, Q.; Cheng, W.; Wang, J.; Feng, Y.; Chai, J.* “Crystal structure of the FTO protein reveals basis for its substrate specificity” Nature 2010, 464, 1205-1209.


Prior to Independent Career

  1. Chou, T.; Dong, H.; Zhang, X.; Lei, X.; Hartung, J.; Zhang, Y.; Lee, H. L.; Wilson, R. M.; Danishefsky, S. J. * “Multifaceted Cytoprotection by Synthetic Polyacetylenes Inspired by the Ginseng-derived Natural Product Panaxytriol” Proc. Natl. Acad. Sci. USA 2011, 108, 14336-14341.
  2. Lee, L. S.; Stephenson,  K. K.;  Fahey, J. W.; Parsons, T. L.;  Lietman, P. S.;  Andrade, A. S.;  Lei, X. Yun, H.; Soon, G.H.; Shen, P.; Danishefsky, S. J.*; Flexner, C.* Induction of Chemoprotective Phase 2 Enzymes by Ginseng and its Components” Planta Med. 2009; 75, 1129-1133
  3. Lei, X.; Danishefsky, S. J.* “Efficient Synthesis of a Novel Resorcyclide as Anticancer Agent Based on Hsp90 Inhibition” Adv. Synth. Catal. 2008, 350, 1677-1681
  4. Lei, X.; Dai, M.; Hua, Z.; Danishefsky, S. J.* “Biomimetic Total Synthesis of Tricycloillicinone and Mechanistic Studies Toward the Rearrangement of Prenyl Phenyl Ethers” Tetrahedron Lett. 2008, 49, 6383-6385
  5. Ng, F.; Yun, H.; Lei, X.; Danishefsky, S. J.; Fahey, J.; Stephenson, K.; Flexner, C.; Lee, L.* “(3R,9R,10R)-Panaxytriol: a molecular-based nutraceutical with possible application to cancer prevention and treatment” Tetrahedron Lett. 2008, 49, 7178-7179
  6. Peng, L. F.; Kim, S. S.; Matchacheep, S.; Lei, X.; Su, S.; Lin, W.; Runguphan, W.; Choe, W. H.; Sakamoto, N.; Beeler, A. B.; Porco, J. A., Jr.; Schreiber, S. L.* and Chung, R. T.* “Identification of Novel Epoxide Inhibitors of HCV Replication Using High-Throughput Screening.” Antimicrob. Agents Chemother. 2007, 51, 3756-3759.
  7. Lei, X.; Porco, J. A., Jr.* “Total Synthesis of the Diazobenzofluorene Antibiotic (-)-Kinamycin C.” J. Am. Chem. Soc. 2006, 128, 14790-14791. (News story describing this work was highlighted in Chem. & Eng. News 2006, 45, 9.)
  8. Porco, J. A., Jr.*; Su, S.; Lei, X.; Bardhan, S.; Rychnovsky, S. D. “Total Synthesis and Structure Assignment of (+)-Hexacyclinol” Angew. Chem. Int. Ed. 2006, 45, 5790-5792; Angew. Chem. 2006, 118, 5922-5924. (News stories describing this work were reported in Chem. & Eng. News 2006, 31, 11 and Nature 2006, 442, 492-493)
  9. Lei, X.; Zaarur, N.; Sherman, M. Y.; Porco, J. A., Jr.* “Stereocontrolled Synthesis of a Complex Chemical Library via Elaboration of Angular Epoxyquinol Scaffolds.” J. Org. Chem. 2005, 70, 6474-6483.
  10. Su, S.; Aquilano, D.; Arumugasamy, J.; Beeler, A. B.; Eastwood, E. L.; Giguere, J. R.; Lan, P.; Lei, X.; Min, G. K.; Yeager, A. R.; Zhou, Y.; Panek, J. S.; Snyder, J. K.; Schaus, S. E.; Porco, J. A., Jr.* “Convergent Synthesis of a Complex Oxime Library Using Chemical Domain Shuffling.” Org. Lett. 2005, 7, 2751-2754.
  11. Lei, X.; Porco, J. A., Jr.* “Synthesis of a Polymer-Supported Anthracene and Its Application as a Dienophile Scavenger.” Org. Lett. 2004, 6, 795-798.
  12. Lei, X.; Johnson, R. P.; Porco, J. A., Jr.* “Total Synthesis of the Ubiquitin-Activating Enzyme Inhibitor (+)-Panepophenanthrin.” Angew. Chem. Int. Ed. 2003, 42, 3913-3917; Angew. Chem. 2003, 115, 4043-4047. (This publication was highlighted as a “Hot Paper”.)



  1. Lei, X.; Li, Q.; Dong, T. CN 201611097411.2
  2. Lei, X.; Liao, D.; Yang, S. CN 201510574855.X
  3. Lei, X.; Liao, D.; Yang, S. CN 201510574855.X
  4. Lei, X.; He, S.; Li, C.; Dong, T. “Sesquiterpenoids” PCT/CN2014/076123
  5. Danishefsky, S. J.; Yun, H.; Chou, T.; Lei, X.; Sames, D. “Compounds and methods for treating cancer or neurotrophic disorder.” US2011/0124690
  6. Danishefsky, S. J.; Chou, T.; Lei, X.; Yun, H.; Ng, F.; Hartung, J.; Sames, D. “Compounds, compositions and methods for reducing toxicity and treating or preventing diseases.”    PCT Int. Appl. 2010, WO2010025272
  7. Danishefsky, S. J.; Chou, T.; Lei, X. “Compounds, compositions and methods for treating or preventing diseases.” PCT Int. Appl. 2009, WO2009105123
  8. Cottarel, G.; Gardner, T.; Lei, X.; Porco, J.; Schaus, S.; Wierzbowski, J. “Compositions and methods for potentiating antibiotic activity using an ATP receptor antagonist, coumarin, flavone, or terpene” PCT Int. Appl., 2008, WO2008019292
  9. Danishefsky, S. J. Lei, X.; Yun, H.; Chou, T. “Compositions and methods using a panaxytriol  compound in combination with a tubulin-binding drug for treating cancer or a neurotrophic disorder.”  PCT Int. Appl. 2008, WO 2008103916


Invited Lectures

  1. RACI National Centenary Conference, Melbourne, Australia, 2017
  2. Tetrahedron Symposium, Hungary, 2017
  3. Swiss Lecture Tour, Switzerland, 2017
  4. UCSF, 2017
  5. KAIST School of Molecular Science BK21 Symposium, South Korea, 2017
  6. CSJ Annual Conference, Tokyo, Japan, 2017
  7. ACBI Conference, Ho Chi Minh City, 2017
  8. ACP meeting in South Korea, 2016
  9. China-Thailand workshop on natural product and drug discovery, Thailand, 2016
  10. 27th European Colloquium of Heterocyclic Chemistry, Amsterdam, 2016
  11. 21st  iCeMS International SymposiumEmerging Science for Unlocking Cell's Secrets”, Kyoto, 2016
  12. RIKEN, Japan, 2016
  13. University of Tokyo, Japan, 2016
  14. Osaka University, Japan, 2016
  15. University of Hong Kong, 2016
  16. Hong Kong University of Science and Technology, 2016
  17. 9th Sino-German Frontiers of Science Symposium, Shenzhen, 2016
  18. University of California at Davis, USA, 2016
  19. IUPAC Congress, South Korea, 2015
  20. CSJ Symposium, Japan, 2015
  21. Sichuan University, 2015
  22. Chongqing University, 2015
  23. Xiamen University, 2014
  24. Sino-Japan Workshop on Chemical Biology, Beijing, 2014
  25. Gordon Research Conference on Heterocyclic Compounds, USA, 2014
  26. CGC Symposium on Chemical Biology by Max-Planck-Institute, Dortmund, 2014
  27. Keystone Conference on Cell Death, New Mexico, USA, 2014
  28. Asian Core Program Meeting on Chemical Biology, Philippines, 2014
  29. The Croucher Foundation Advanced Study Institute for Chemical Biology, Hong Kong, December 15-17, 2013
  30. National University of Singapore, 2013
  31. Nanyang Technological University, 2013
  32. The International Symposium on Natural Product Chemistry and Chemical Biology, Nagoya, Japan, November 20-23, 2013
  33. The Roche and RSC Chemistry Symposium: leading science for drug discovery, Shanghai, 2013
  34. ICBS 2013: The 2nd Annual Meeting of the International Chemical Biology Society in Kyoto, Japan, 2013
  35. The first Asian conference for “MONODUKURI” Strategy by Synthetic Organic Chemistry (ACMS) in Okinawa, Japan, 2013
  36. Tsinghua University, 2013
  37. Nankai University, 2013
  38. 3rd Annual Chemical BiologySymposium of our Synthetic and Functional Biomolecules Center (SFBC) at Peking University, 2013
  39. “Gao Ji Yu Lecture” Nanjing University, 2013
  40. East China Normal University, 2013
  41. China Pharmaceutical University, 2013
  42. The 7th International Conference on Cutting-Edge Organic Chemistry in Asia, Singapore, 2012
  43. The 4th China-Thailand Workshop on Natural Products and Drug Discovery, Songkla, Thailand, 2012
  44. International Conference of Chemical Biology of Natural Products: Target ID and Regulation of Bioactivity, Kyoto, Japan, 2012
  45. International Symposium on Natural Product Synthesis and Innovative Process Methods for Drug Manufacture, Chongqing, China, 2012
  46. Cell Symposium: Genetics & Chemistry, Boston, USA, 2012
  47. 8th Sino-US Chemistry Professor Conference, Kunming, China, 2012
  48. National Meeting of Chinese Chemistry Society, Chengdu, China, 2012
  49. Oriental Scientific Symposium on Organic Synthesis, Shanghai, China, 2012
  50. National Organic Symposium of China, Nanjing, China, 2011
  51. Lanzhou University, Lanzhou, China, 2011
  52. Second Military Medical University, Shanghai, China, 2011
  53. Nankai University, Tianjin, China, 2011
  54. Pacifichem Congress, Honolulu, December 20th, 2010
  55. ACS National Meeting, Boston, USA, 2010
  56. ESF-COST Conference on Natural Products Chemistry, Biology and Medicine III, Acquafredda di Maratea, Italy, 2010
  57. Peking University, Beijing, China, 2010
  58. 6th Sino-US Chemistry Professor Conference, Hangzhou, China, 2010
  59. 5th Sino-US Chemistry Professor Conference, Lanzhou, China, 2009



  • NNSFC-Distinguished Young Investigator (21625201), 2017-2021, PI
  • NNSFC (21561142002), 2015-2018, PI
  • National High Technology Projects 973 (2015CB856200), 2015-2019, Co-PI
  • NNSFC (21472010), 2015-2017, PI
  • NNSFC (91313303), 2014-2015, Co-PI
  • National High Technology Projects 973 (2012CB837400), 2012-2016, Chief Scientist
  • NNSFC-Outstanding Young Investigator (20122209), 2013-2015, PI
  • NNSFC (21072150), 2011-2013, PI
  • Program for New Century Excellent Talents in University (NCET-10-0614), 2011-2013, PI
  • National High Technology Projects 863 (2008AA022317), 2009-2011, PI
  • NNSFC (20802050), 2009-2011, PI



  • 2014-, “Introduction to Chemical Biology” for undergraduate students, Peking University
  • 2014-, “Organic Chemistry” for undergraduate students, Peking University
  • 2012-, PTN program “Chemical Biology”
  • 2009-2012, Tianjin University “Medicinal Chemistry” for graduate students
  • 2009-2012, Tianjin University “Advanced Organic Chemistry” for undergraduate students