Research |
Yefeng TANG, PhD

Yefeng TANG, PI

Tenured Full Professor

Professor Tang earned his bachelor's degree in Chemistry from Lanzhou University in 1999, followed by a master's degree in Medicinal Chemistry from the Institute of Materia Medica at the Chinese Academy of Medical Sciences. From 2003 to 2006, he completed his Ph.D. in Organic Chemistry at Peking University under the supervision of Professors Zhen Yang and Jia-Hua Chen. He then conducted postdoctoral research (2006–2009) in the laboratory of Professor K. C. Nicolaou at The Scripps Research Institute in the United States. Since June 2010, he has been conducting independent research at Tsinghua University, where he held positions as an assistant professor, tenured associate professor, and tenured full professor consecutively. His research group specializes in natural product synthesis, chemical biology, and medicinal chemistry, with a particular focus on structurally novel and biologically significant natural products. By developing innovative synthetic strategies and methodologies, his team has achieved the efficient and diverse synthesis of over 100 natural molecules. These bioactive compounds have been further applied in drug discovery and chemical biology studies, which leads to the identification of some new drug candidates and targets. Prof. Tang has published nearly 100 papers in high-impact journals, including Cell Research, Accounts of Chemical Research, Journal of the American Chemical Society, Angewandte Chemie International Edition, ACS Catalysis, and Chemical Science. He holds five patents and has co-authored two textbooks. Additionally, he serves on the editorial boards of Chinese Journal of Medicinal Chemistry, Pharmaceutical Science Advance, and Frontiers in Chemistry.

Honors and Awards


Outstanding Staff Member of Tsinghua University (2025)

Excellent Undergraduate Theses Supervisors of Beijing General Colleges and Universities (2023)

The Ministry of Education of Yangtze River Scholar Professor (2022)

Excellent doctoral thesis supervisor of Tsinghua University (2021, 2018)

Tsinghua University Online Teaching Excellence Award (2020)

Thieme Chemistry Journals Award (2019)

The First Prize of Science and Technology Award of Chinese Pharmaceutical Society (2019)

The Second Prize of National Natural Science Award (2016)

Guangdong Province Science and Technology Progress Award (2015)

Tsinghua-Bayer Investigator Award (2014)

Tsinghua-Janssen Investigator Award (2011-2015)

Research Interests


The Tang Laboratory is dedicated to natural product-inspired synthetic chemistry, medicinal chemistry, and chemical biology. Our research centers on biologically active molecules—particularly natural products and drug-like compounds—as key platforms for innovative discovery. By developing efficient, practical, and sustainable synthetic methodologies, we enable rapid, scalable, and diverse access to these molecules, facilitating their exploration in drug development and biomedical applications. Currently, the research directions in the Tang laboratory include:

1) Total Synthesis of Natural Products---Targeting molecules with distinctive scaffolds, promising bioactivity, and unexplored biosynthetic pathways.

2) Synthetic methodologies---Developing novel reactions to efficiently construct privileged structures in natural products and drugs.

3) Medicinal Chemistry---Rational design, synthesis, and biological evaluation of small-molecule agents with antiviral, anticancer, and neuroprotective properties.

4) Bioorthogonal Chemistry---Creating new bioorthogonal reactions and leveraging them as tools to probe and manipulate biological system

Major Scientific Achievements


1) Guided by the research philosophy that integrates biomimetic synthesis with rational design, we have systematically developed efficient and diversified synthetic approaches to more than 10 classes of relevant natural products, including Xanthane-type sesquiterpenes, Stemona alkaloids, Cytochalasins. Plakortide polyketides, Hydroquinone/quinone-sesquiterpenoid hybrids, and others (Fig. 1). Our efforts have culminated in the total synthesis of over 100 target molecules, providing critical material support for systematic investigation of their biological functions and therapeutic potential.

Figure 1：Total syntheses of natural products completed in the Tang group

               
2）   Centered on "triazole ring-opening chemistry" (Fig. 2) and "   ring strain-driven expansion and rearrangement reactions   " (Fig. 3), we have developed a series of novel and efficient synthetic methodologies   , which enable the rapid construction of various privileged structures of natural products or drugs, thereby providing key technical support for total synthesi   s   and drug discovery.  
 

Figure 2：Synthetic methodologies based on the ring-opening chemistry of triazoles


   Figure 3：Strain-driven ring expansion and rearrangement reactions

               

3) Based on inspiration from natural product synthesis, we have established several unique strain-driven bioorthogonal reactions (Fig. 4), some of which have been successfully applied to in vitro protein labeling and live cell imaging.

Figure 4: Nature-inspired bioorthogonal reactions

               

4) We have developed two classes of small molecules with great potential as drug candidates, including a class of tryptophanyl-tRNA synthetase (TrpRS) inhibitors with anti-Mycobacterium tuberculosis activity (Fig. 4) and a class of nicotinamide mononucleotide adenosyltransferase (NMNAT) agonists with neuroprotective effect.

Figure 5: Development of novel anti-tuberculosis agent


Figure 6：Development of novel NAMPT agonists


Selected Publications

1. Li, Y.#; Zhang, J.#; Chen, Y.; Pang, J.; Chen, Y.; Tang, Y. F.* Dyotropic Rearrangement of β-Lactams: Reaction Development, Mechanistic Study, and Application to the Total Syntheses of Tricyclic Marine Alkaloids. Angew. Chem. Int. Ed. 2025, 64, e202414985.

2. Zhang, J. Y.#; Kong, W. Y.#; Guo, W. T.; Tantillo, D. J.*; Tang, Y. F.* Combined Computational and Experimental Study Reveals Complex Mechanistic Landscape of Brønsted Acid-Catalyzed Silane-Dependent P=O Reduction. J. Am. Chem. Soc. 2024, 146, 13983-13999.

3. Yang, H. Z.#; Zhang, J. Y.#; Zhang, S.; Xue, Z. W.; Hu, S. K.; Chen, Y.; Tang, Y. F.* Chiral Bisphosphine-Catalyzed Asymmetric Staudinger/aza-Wittig Reaction: An Enantioselective Desymmetrizing Approach to Crinine-type Amaryllidaceae Alkaloids. J. Am. Chem. Soc. 2024, 146, 14136-14148.

4. Hu, S. K.; Tang, Y. F.* Enantioselective Total Synthesis of Dysiherbols A, C, and D. J. Am. Chem. Soc. 2022, 144, 19521-19531.

5. Yao, H.#; Liu, M. H.#; Wang, L. B.#; Zu, Y. M.#; Wu, C.; Li, C. Y.; Zhang, R. X.; Lu, H. G.; Li, F. F.; Xi, S.; Chen, S. Q.; Gu, X. Y.; Liu, T. Y.; Cai, J.; Wang, S. R.; Yang, M. J.; Hua, L.; Xing, G. G.; Tang, Y. F.*; Wang, G. L.* Discovery of small-molecule activators of nicotinamide phosphoribosyltransferase (NAMPT) and their preclinical neuroprotective activity. Cell Res. 2022, 32, 570-584.

6. Bao, R. Y.; Zhang, H. Y.; Tang, Y. F.* Biomimetic Synthesis of Natural Products: A Journey To Learn, To Mimic, and To Be Better. Acc. Chem. Res. 2021, 54, 3720–3733.

7. Guo, Z.; Bao, R. Y.; Li, Y. H.; Li, Y. S.; Zhang, J. Y.; Tang, Y. F.* Tailored Synthesis of Skeletally Diverse Stemona Alkaloids through Chemoselective Dyotropic Rearrangements of β-Lactones. Angew. Chem. Int. Ed. 2021, 60, 14545–14553.

8. Lei, X. Q.; Li, Y. H.; Lai, Y.; Hu, S. K.; Qi, C.; Wang, G. L.*; Tang, Y. F.* Strain-Driven Dyotropic Rearrangement: A Unified Ring-Expansion Approach to α-Methylene-γ-butyrolactones. Angew. Chem. Int. Ed. 2021, 60, 4221–4230.

9. Bao, R. Y.; Tian, C.; Zhang, H. Y.; Wang, Z. G.; Dong, Z.; Li, Y. H.; Gao, M. H.; Zhang, H. L.; Liu, G.*; Tang, Y. F.* Total Syntheses of Asperchalasines A–E. Angew. Chem. Int. Ed. 2018, 57, 14216-14220.

10. Li, Q. G.#; Zhao, K.#; Peuronen, A.; Rissanen, K.; Enders, D.*; Tang, Y. F.* Enantioselective Total Syntheses of (+)-Hippolachnin A, (+)-Gracilioether A, (-)-Gracilioether E and (-)-Gracilioether F. J. Am. Chem. Soc. 2018, 140, 1937–1944.

11. Feng, J.; Lei, X. Q.; Bao, R. Y.; Li, Y. H.; Xiao, C. Q.; Hu, L. H.; Tang, Y. F.* Enantioselective and Collective Total Syntheses of Xanthanolides. Angew. Chem. Int. Ed. 2017, 56, 16323–16327.

12. Feng J.#; Lei, X. Q.#; Guo, Z.; Tang, Y. F.* Total Synthesis of Homodimericin A. Angew. Chem. Int. Ed. 2017, 56, 7895–7899.

13. Tian, C.; Lei, X. Q.; Wang, Y. H.; Dong, Z.; Liu, G.*; Tang, Y. F.* Total Syntheses of Periconiasins A-E. Angew. Chem. Int. Ed. 2016, 55, 6992–6996.

14. Shang, H.#; Liu, J. H.#; Bao, R. Y.; Cao, Y. Zhao, K.; Xiao, C. Q.; Zhou, B.; Hu, L. H.*; Tang, Y. F.* Biomimetic Synthesis: Discovery of Xanthanolide Dimers. Angew. Chem. Int. Ed. 2014, 53, 14494–14498.

15. Shang, H.#; Wang, Y. H.#; Tian, Y. Feng, J.; Tang, Y. F.* The Divergent Synthesis of Nitrogen Heterocycles by Rhodium(II)-Catalyzed Cycloadditions of 1-Sulfonyl 1,2,3-Triazoles with 1,3-Dienes. Angew. Chem. Int. Ed. 2014, 53, 5662–5666.

16. Fu, J. K.; Shang, H.; Wang, Z. F.; Chang, L.; Shao, W. B.; Yang, Z.*; Tang Y. F.* Gold-Catalyzed Rearrangement of Allylic Oxonium Ylides: Efficient Synthesis of Highly Functionalized Dihydrofuran-3-ones. Angew. Chem. Int. Ed. 2013, 52, 4198–4202.

17. Ren, W. W.; Bian, Y. C.; Zhang, Z. Y.; Shang, H.; Zhang, P. T.; Chen, Y. J.; Yang, Z.*; Luo T. P.*; Tang Y. F.* Enantioselective and Collective Syntheses of Xanthanolides by Controllable Dyotropic Rearrangement of cis-b-Lactones. Angew. Chem. Int. Ed. 2012, 51, 6984–6988.

18. Xiao, Q.#; Ren W. W.#; Chen, Z. X.; Sun, T. W.; Li, Y.; Ye, Q. D.; Gong, J. X.; Meng, F. K.; You, L.; Liu, Y. F.; Zhao, M. Z.; Xu, L. M.; Shan, Z. H.; Shi, Y.; Tang, Y. F.*; Chen, J. H.*; Yang Z.* Diastereoselective Total Synthesis of (+)-Schindilactone A. Angew. Chem. Int. Ed. 2011, 50, 7373–7377.

19. Nicolaou, K. C.*; Tang, Y. F.; Wang, J. H. Total Synthesis of Sporolide B. Angew. Chem. Int. Ed. 2009, 48, 3501–3505.

20. Nicolaou, K. C.*; Tang, Y. F.; Wang, J. H. Total Synthesis and Antibacterial Properties of Carbaplatensimycin. J. Am. Chem. Soc. 2007, 129, 14850-14851.


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