Dr. Zhu-Jun Yao currently serves as a University Distinguished Professor at the School of Chemistry and Chemical Engineering. He received his BS degree at Fudan University in 1990, and MS & PhD degrees at the Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences in 1992 and 1995, respectively. He carried out his postdoc training at the National Institute of Health (NIH) of United States during 1996-1999.

Dr. Yao's research interests include synthetic natural product chemistry and chemical biology. He has published 5 books, more than 200 peer-review journal publications and 20 patents in these fields, and has received a sound number of famous fundings and awards for the outstanding scholars, including Hundred Talents Program of Chinese Academy of Sciences, NSFC Fund for Outstanding Young Investigator, Leading Talents of Shanghai Municipality, Chinese Chemical Society Award for Creative Work in Organic Synthesis, Excellece of Chemistry in Asia by Eli Lilly, Special Allowance of State Council, Natural Science Award of Chinese Academy of Science, etc.

Dr. Yao is also an active member of Chinese Chemical Society, American Chemical Society, and International Union of Pure and Appied Chemistry (IUPAC). He also serves as a long-term duty in the Supervisory Committee of National Natural Science Foudation of China (NSFC).

Sept 1995 - Sept 1996, Assistant Research Fellow, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences;

Sept 1996 - Sept 1999, NIH Fogarty International Visiting Fellow, NCI Division of Basic Sciences, NIH, USA.

Sept 1999 - Dec 2009, Research Fellow, Principal Investigator, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences;

Sept 2008 - date, University Distinguished Professor, School of Chemistry and Chemical Engineering, Nanjing University.

Dr. Zhu-Jun Yao's research team mainly works in the field of synthetic natural product chemistry, medicinal chemistry and chemical biology. 

Utilizing innovative synthetic methodologies established in the total syntheses, they develop new chemical entities of medicinal interest and explore the mechanisms of biological action using chemical biology principles. Recent achievements by this group include (1) completion of the first total syntheses of cyclomarin, chlorofusin, chloptosin, clavulactone, lannotinidine B, plumisclerin A and several other complex bioactive natural products; (2) invention of AA005, an artificial mimicry of cytotoxic acetogenin exhibiting high inhibitory potency against the proliferation of various cancer cells and significant action selectivity between human cancerous and healthy cells, and explanation of the mechanisms associated with the unique cell selectivity; (3) short and high-yielding total syntheses of the famous alkaloids camptothecin (CPT), 10-hydroxycamptothecin and marketed anticancer drug Irinotecan, as well as development of more potent new anticancer derivatives; (4) new economic syntheses of two famous anti-influenza drugs Relenza and Tamiflu from the easily available materials glucono-delta-lactone and amino acids, and the first catalytic asymmetric synthesis of (-)-huperzine A by multifunctional organocatalysis; and (5) development of potent immune-regulating agents from economically available alkaloid sinomenine, a poorly active TCM intergradient.

Fig 1. Illustration of recent synthetic targets and completed total syntheses of bioactive natural products

For more details, please browse Dr. Yao's group webpage at http://hysz.nju.edu.cn/yaozj/.

Dr. Zhu-Jun Yao has published 5 books, more than 200 peer-review journal publications and 20 patents in the fields of synthetic natural product chemistry and chemical biology.

Selected recent publications:

(1) Wang, T.-Y.; Feng, D.-H.; Wang, Y.-K.; Yao, Z.-J. Quick Access to Protoberberine and Tetrahydroprotoberberine Derivatives/Analogues with One-pot Sequential Isochromenylium-mediated Annulation. J. Org. Chem. 2024, (submitted on June 19, 2024).

(2) Mai, Z.-P.; Zhang, B.; Pang, Z.-X.; Shi, J.; Xu, Z.-F.; Huang, B.-B.; Ma, S.-Y.; Jiao, R.-H.; Yao, Z.-J.; Tan, R.-X.; Ge, H.-M. A trans-AT polyketide synthase accomplishes iterative function in the biosynthesis of lankacidin-type natural products. Nat. Synth. 2024 (MS#NATSYNTH-23121423B, accepted on June 6, 2024).

(3) Nong, K.; Zhao, Y.-L.; Yi, S.; Zhang, X.; Wei, S.; Yao, Z.-J. 3-Acyl-4-pyranone as Lysine-residue Selective Bioconjugation Reagent for Peptide and Protein Modification. Bioconjugate Chem.2024, 35, 286-299. (DOI: 10.1021/acs.bioconjchem.3c00447)

(4) Wang, M.; Wang, T.; Qin, X.; Yao, Z.-J. Development of Cyclic N,O-Aminal-Embedded Bis-tetrahydroisoquinoline Analogues as Potential DNA Alkylation Agents. Org. Lett. 2024, 26, 1764-1769. (DOI: 10.1021/acs.orglett.3c04143)

(5) Wang, T.; Wang, Y.; Feng, D.; Wang, M.; Yang, X.; Yao, Z.-J. Isochromenylium/Isoquinolinium-Mediated One-Pot Annulationto Hexahydropyrazinoisoquinolines. Synthesis of Quinocarcinol. Org. Lett. 2023, 25, 8803−8808. (DOI: 10.1021/acs.orglett.3c03368; published on Dec. 6, 2023)

(6) Yi, S.; Wei, S.; Wu, Q.; Wang, H.; Yao, Z.-J. Azaphilones as Activation-Free Primary Amine-Specific Bioconjugation Reagents for Peptides, Proteins and Lipids. Angew. Chem. Int. Ed. 2022, 61(6), e202111783 (DOI: 10.1002/anie.202111783; published on Feb. 1, 2022).

(7) Tang, S.; Wu, Z.; Gao, M.; Li, G.; Yao, Z.-J. Total Synthesis of Suberitines A-D Featuring Tunable Biomimetic Late-Stage Oxidative Dearomatization and Acetalization, Chem. Eur. J. 2022, 28(24), e202200644 (DOI: 10.1002/chem.202200644).

(8)Huang, B.-B.; Lei, K.; Zhong, L.-R.; Yang, X.; Yao, Z.-J. A Unified Total Synthesis of Tetracyclic Diquinane Lycopodium Alkaloids (+)-Paniculatine, (−)-Magellanine and (+)-Magellaninone. J. Org. Chem. 2022, 87, 8685-8696 (DOI: 10.1021/acs.joc.2c00871; accepted on June 3, 2022).

(9) Yu, B.-B.; Yuan, H.; Chen, Y.-C.; Zhou, D.-X.; Gan, Z.-J.; Wang, J.; Li, J.-X.; Yao, Z.-J. Annonaceous Acetogenin Mimic AA005 Inhibits the Growth of TNBC MDA-MB-468 Cells by Altering Cell Energy Metabolism. ChemBioChem 2022, e202200250. (DOI: 10.1002/cbic.202200250; accepted on May 30, 2022).

(10) Gao, M.; ^‡ Yu, B.-B.;^‡ Jia,C.; Yao, Z.-J. Cytotoxic analogues of marine diterpenoid plumisclerin A by shifting the lipophilic branch on the characteristic tricyclic core. Org. Biomol. Chem. 2022, 20, 4553-4558. (^‡These authors contributed equally to this work. DOI: 10.1039/D2OB00539E; accepted on April 12).

(11) Huang, B.-B.;^# Zhao, Y.-L.;^# Lei, K.; Zhong, L.-R.; Yang, X.; Yao, Z.-J. Enantioselective Total Synthesis of (+)-Sieboldine A and Analogues Thereof. Org. Lett. 2022, 24, 7517−7521. (Accepted on October 7, 2022; DOI: 10.1021/acs.orglett.2c02737). (^#These authors contributed equally to this work)

(12) Wang, M.; Yu, B.-B.; Yao, Z.-J. Simplified hybrids of two anticancer bistetrahydroisoquinoline alkaloidsecteinascidin 743 and cribrostatin 4 and inhibitory activity against proliferation of cancer cells. Org. Biomol. Chem. 2022, 20, 8438 - 8442. (DOI: 10.1039/D2OB01707E; accepted on October 11, 2022, first published on October 11, 2022)

(13) Zhong, L.-R.; Huang, B.-B.; Yang, X.-L.; Wang, S.-z.; Yao, Z.-J. Concise Unified Access to (−)-8-Deoxy-13-dehydroserratinine, (+)-Fawcettimine, (+)-Fawcettidine, and (−)-8-Deoxyserratinine Using a Direct Intramolecular Reductive Coupling. Organic Letters 2021, 23, 3578−3583.

(14) Xie, J.;^† Zhu, G.;^† Gao, M.;^† Xi, J.; Chen, G.; Ma, X.; Yan, Y.; Wang, Z.; Xu, Z.-J.; Chen, H.-J.; Hao, H.-D.; Zhang, Y.; Yao, Z.-J.; Zhu, J. Artemisinin derivative ART1 induces ferroptosis by targeting the HSD17B4 protein essential for lipid metabolism and direct induction of lipid peroxidation. CCS Chemistry 2021, 3, 664–677 (^†These authors contributed equally to this work).

(15) Qiao, J.-H.; Zhao, W.-X.; Liang, Y.; Yao, Z.-J.; Wang, S.-z. Diastereospecific Access to Tetracyclic Eight-Membered Lactams through a Dearomative Heck Reaction and an Alkylative Ring-Opening Driven by the Photoexcited Spiroindolines. Chem. Eur. J. 2021, 27, 6308–6314.

(16) Zhong, L.-R.; Yang, Y.; Huang, B.-B.; Yao, Z.-J. An eight-step total synthesis of pyrroloquinolone-type Lycopodium alkaloid via a tandem annulation approach. Chin. J. Chem. 2020, 38, 1560-1564. 

(17) Shan, H.-z; Cao, Y.; Xiao, X.-h.; Liu, M.; Wu, Y.-z.; Zhu, Q.; Xu, H.-z.; Lei, H.; Yao, Z.-J.;, Wu, Y.-L. YL064 activates proteasomal-dependent degradation of c-Myc and synergistic with ABT-199 in diffuse large B cell lymphoma. Signal Transduction and Targeted Therapy 2020, 5, 116.

(18)Gao, M.; Wang, Y.-C.; Yang, K.-R.; He, W.; Yang, X.-L.; Yao, Z.-J. Enantioselective Total Synthesis of (+)-Plumisclerin A. Angew. Chem. Int. Ed. 2018, 57, 13313-13318. 

(19) Zhang, L.; Wang, Y.; Yao, Z.-J.; Wang, S.-z.; Yu, Z.-X. Kinetic or Dynamic Control on a Bifurcating Potential Energy Surface? An Experimental and DFT Study of Gold-Catalyzed Ring Expansion and Spirocyclization of 2-Propargyl-β-tetrahydrocarbolines. J. Am. Chem. Soc. 2015, 137, 13290–13300. 

(20) Yu, S.-Y.; Zhang, H.; Gao, Y.; Mo, L.; Wang, S.-z.; Yao, Z.-J. Asymmetric Cascade Annulation Based on Enantioselective Oxa Diels−Alder Cycloaddition of in Situ Generated Isochromenyliums by Cooperative Binary Catalysis of Pd(OAc)₂ and (S)-Trip. J. Am. Chem. Soc. 2013, 135, 11402−11407.

(21) Ge, H. M.; Zhang, L.-D.; Tan, R. X.; Yao, Z.-J.Protecting Group-Free Total Synthesis of (-)-Lannotinidine B. J.Am. Chem. Soc. 2012, 134, 12323-12325.

(22) Yang, Z.-Y.; Liao, H.-Z.; Sheng, K.; Chen, Y.-F.; Yao, Z.-J. Enantioselective Total Synthesis of Marine Diterpenoid Clavulactone. Angew. Chem. Int. Ed. 2012, 51, 6484-6487.

For more details, please browse Dr. Yao's group webpage at http://hysz.nju.edu.cn/yaozj/.

1. Introduction of Life Chemistry, the first semester of univeristy freshman

2. Advances in Organic Chemistry and Related Fields, the first semester of grade 4 (undergraduate)

3. Mordern Organic Synthesis, the second semester of first year of graduate students

Current members of Dr. Yao's group include one professor, two associate professors, one associate research fellow, an administrative assistant, one postdoctoral fellow, fourteen Ph.D. candidates and three graduate student.

For more details, please browse Dr. Yao's group webpage at http://hysz.nju.edu.cn/yaozj/.