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Dr. Yi Li received his B.S. degree in pharmacy from Wuhan University in 2009. He obtained his Ph.D. degree in medicinal chemistry from Shanghai Institute of Materia Medica, Chinese Academy of Sciences in 2014 and continued to work as a research assistant until 2016. Then he was selected into the Young Talented Program and worked as the project leader of medicinal chemistry in WuXi DDSU. After completing postdoc training at University of Texas Medical Branch from 2018 to 2022, Dr. Li joined Shanghai Institute of Materia Medica and Zhongshan Institute for Drug Discovery as a Professor and Principal Investigator. His current research focuses on small-molecule drug discovery and development of novel synthetic methodology.

1. The discovery of innovative drug candidates

2. The development of novel synthetic methodologies

1. Developed innovative drug candidates for some diseases including cancer, diabetes and obesity.

2. Identified a novel BRD4 BD1 selective probe targeting a unique, previously unreported non-acetylated lysine binding site.

3.Developed efficient strategies for the asymmetric synthesis of a series of structurally important chiral molecules.

1. Z. Liu^#, Y. Li^#, H. Chen, H.-T. Lai, P. Wang, S.-Y. Wu, E. A. Wold, P. G. Leonard, S. Joseph, H. Hu, C.-M. Chiang, A. R. Brasier^*, B. Tian^*, J. Zhou^*, Discovery, X-ray Crystallography, and Anti-Inflammatory Activity of Bromodomain-Containing Protein 4 (BRD4) Inhibitors Targeting a Distinct New Binding Site, J. Med. Chem. 2022, 65, 2388-2408. (Cover Article and Selected as the Special Issue “Epigenetics 2022”)

2. Y. Li^#, J. Chen^#, A. Bolinger, H. Chen, Z. Liu, Y. Cong, A. R. Brasier, I. V. Pinchuk, B. Tian^*, J. Zhou^*, Target-Based Small Molecule Drug Discovery towards Novel Therapeutics for Inflammatory Bowel Diseases, Inflamm. Bowel Dis. 2021, 27, S38–S62.

3. Y. Li, M. Xu^*, Applications of Asymmetric Petasis Reaction in the Synthesis of Chiral Amines, Acta Chim. Sinica 2021, 79, 1345.

4. Y. Li^#, Z. Liu^#, G. Aglyamova^#, J. Chen, H. Chen, M. Bhandari, M. A. White, G. Rudenko^?, J. Zhou^?, Discovery of Phenanthridine Analogues as Novel Chemical Probes Disrupting the Binding of DNA to ΔFosB Homodimers and ΔFosB/JunD Heterodimers, Bioorg. Med. Chem. Lett. 2020, 30, 127300.

5. Y. Li^#, B. Liu^#, M. Xu^*, Rhodium-Catalyzed Enantioselective Alkenylation of Cyclic Ketimines: Synthesis of Multifunctional Chiral α,α-Disubstituted Allylic Amine Derivatives, Org. Lett. 2018, 20, 2306. (Highlighted by Synfacts, 2018, 14, 0596)

6. Y. Li^#, Y. Yu^#, M. Xu^*, Simple Open-Chain Phosphite-Olefin as Ligand for Rh-Catalyzed Asymmetric Arylation of Cyclic Ketimines: Enantioselective Access to gem-Diaryl α-Amino Acid Derivatives, ACS Catal. 2016, 6, 661. (Highlighted by The Journal Homepage).

7. H. Wang^#, Y. Li^#, M. Xu^*, Rhodium-Catalyzed Highly Enantioselective Arylation of Cyclic Diketimines: Efficient Synthesis of Chiral Tetrasubstituted 1,2,5-Thiadiazoline 1,1-Dioxides, Org. Lett. 2014, 16, 3962. (Highlighted by Synfacts, 2014, 10, 1044)

8. Y. Li, M. Xu^*, Rhodium-Catalyzed Asymmetric Tandem Cyclization for Efficient and Rapid Access to Underexplored Heterocyclic Tertiary Allylic Alcohols Containing a Tetrasubstituted Olefin, Org. Lett. 2014, 16, 2712. (Highlighted by Synfacts, 2014, 10, 0680)

9. Y. Li, M. Xu^*, Simple Sulfur-Olefins as New Promising Chiral Ligands for Asymmetric Catalysis, Chem. Commun. 2014, 50, 3771. (Feature Article, Selected as Cover Article)

10. Y. Li, D. Zhu, M. Xu^*, A new Versatile Approach to Enantioenriched 3-Hydroxyoxindoles, 1, 3-Dihydroisobenzofuran and 3-Isochromanone Derivatives by Rhodium-Catalyzed Asymmetric Arylation/Cyclization Sequence, Chem. Commun. 2013. 49, 11659. (Highlighted by Synfacts, 2014, 10, 0285; ChemComm Editor’s Choice)

11. Y. Li, M. Xu^*, Lewis Acid-Catalyzed Intramolecular Aza-Friedel-Crafts Reaction of N-tert-Butanesulfinyl Imines: Efficient Synthesis of Optically Active 9-Aminoflourene Derivatives, Asian J. Org. Chem. 2013, 2, 50-53. (Selected as Cover Article; One of the most-accessed Asian J. Org. Chem. articles in April 2013)

12. Y. Li, M. Xu^*, Lewis Acid-Promoted Highly Diastereoselective Petasis Borono-Mannich Reaction: Efficient Synthesis of Optically Active β, γ-Unsaturated α-Amino Acids, Org. Lett. 2012, 14, 2062. (Highlighted by Synfacts, 2012, 8, 0744)

14. Y. Li, D. Ji, M. Xu^*, Highly Diastereoselective Friedel-Crafts Reaction of Arenes with N-tert-Butanesulfinylimino Ester towards the Efficient Synthesis of α-Arylglycines, Org. Biomol. Chem. 2011, 9, 8452.