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Chemical Synthesis:

Chemical Synthesis plays a fundamental role in the pharmaceutical industry and drug discovery process. Usually, the natural products serve as a source of raw material for novel drug discovery, a chemical modification remains imperative to enhance the efficacy/safety profile of a new drug. Chemical Synthesis enabled the drug discovery of many breakthrough therapies over the past years. Facing the increasing challenges in the pharmaceutical development, Advanced Chemical Synthesis strategies are required to drive the discovery of various medicines.

 

The Synthesis methods and process access to previously unattainable chemical compound and inspire new concepts as novel drug design to transform the practice of drug discovery and development.

 

Our group proposed a new strategy of proton-shuttling catalysis (i.e. space regulation of protons) and found a series of highly asymmetric reactions, and then designed multi-site catalytic intermediates to participate in the selective protonation (i.e. time regulation of protons) to unlock a series of unknown chemical reactions. The concept of proton selective migration is applied to the migration reactions of other research groups, which provides new ideas and technical method for the synthesis of specific fragments and skeletons.


(1) Development of proton migration reagent

(2) Study on reactive intermediates at multiple sites

(3) Study on group migration reaction

(4) Research on the application of synthetic methodology to targeted antitumor Drug.


The Latest Progresses of Chemical Synthesis

Technology

Chen, J.; Huang, Y.*, Asymmetric Catalysis with N-heterocyclic Carbenes as Non-covalent Chiral Templates. Nat. Commun. 2014, 5, 3437.

Yuan, P.; Chen, J.*; Zhao, J.*; Huang, Y.*, Enantioselective Hydroamidation of Enals by Trapping of a Transient Acyl Species. Angew. Chem. Int. Ed. 2018, 57, 8503.

Wang,Z.; Li, X.; Huang, Y.*, Direct α-Vinylidenation of Aldehydes and Subsequent Cascade Gold and Amine Catalysts Work Synergistically. Angew. Chem. Int. Ed. 2013, 42, 14219. Luo, C.;

Wang, Z.; Huang, Y.*, Asymmetric Intramolecular α-Cyclopropanation of Aldehydes Using a Donor/Acceptor Carbene Mimetic. Nat. Commun. 2015, 6, 10041.

Technology
Technology

Wang, L.; Wu, F.; Chen, J.; Nicewicz, D. A.*; Huang, Y.*, Visible Light Mediated [4+2] Cycloaddition of Styrenes Synthesis of Tetralin Derivatives. Angew. Chem. Int. Ed. 2017, 56, 6896.

Wu, F.; Wang, L.; Chen, J.*; Nicewicz, D. A.*; Huang, Y.*, Direct Synthesis of Polysubstituted Aldehydes via Visible-Light-Catalysis. Angew. Chem. Int. Ed. 2018, 57, 2174.

Wang, Z.; He, Z.; Zhang, L.; Huang, Y.*, Iridium-Catalyzed Aerobic α,β-Dehydrogenation of γ,δ-Unsaturated Amides and Acids: Activation of Both α- and β-C–H bonds through an Allyl–Iridium Intermediate. J. Am. Chem. Soc., 2018, 140, 735.

He, Z.; Song, F.; Sun, H.; Huang, Y.*, A Transition-Metal-Free Suzuki-Type Cross-Coupling Reaction of Benzyl Halides and Boronic Acids via 1,2-Metallate Shift. J. Am. Chem. Soc., 2018, 140, 2693.

Technology
Technology

Pan, P.; Chen, J. et al. Huang, Y.*; Hou, T.*, Structure-Based Drug Design and Identification of H2O-Soluble and Low Toxic Hexacyclic Camptothecin Derivatives with Improved Efficacy in Cancer and Lethal Inflammation Models in Vivo. J. Med. Chem. 2018, 61, 8613.

Pan, P.; Yu, H. et al. Huang, Y.*; Hou, T.*, Combating Drug-Resistant Mutants of Anaplastic Lymphoma Kinase with Potent and Selective Type‑I 1/2 Inhibitors by Stabilizing Unique DFG-Shifted Loop Conformation. ACS Cent. Sci. 2017, 3, 1208.

 

Peptide Drug Development
 

about

Poly-Peptide played a notable role in medical therapeutics practice since insulin. Peptides represent a class of pharmaceutical compounds, molecularly between small molecules and proteins. There are over 60 peptide drugs got approved in the United States and other major markets. And there are more peptides continue to forward to clinical development and got approved recently such as Liraglutide and Somaglutide.
 

The discovery of Peptide drug has diversified from endogenous human peptides to a broader range of other natural sources. One advantage of peptides treatment is that provide an opportunity for therapeutic intervention that closely mimics natural pathways and physiological functions.
 

Our research areas mainly include four aspects: methodological research on stabilizing the secondary structure of peptides, research on therapeutic targets, modulation of microbial virulence and research on anti-infection treatment, and peptide self-assembling materials. The laboratory has self-contained platform technologies, including solid-phase peptide synthesis technology, photocatalytic reaction technology, peptide in vitro characterization technology, high-throughput fluorescence screening technology, mass spectrometry technology, cell biology technology, small animal fluorescence imaging technology, and establishment technology of mouse models of tumors and other diseases, in vivo detection and immunohistochemistry, etc.


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