Yang Yaxi
Medical School
University of Chinese Academy of Sciences
Shanghai
Language: Chinese, English
Contact
Drug Design Synthesis Pharmacology Bioactivity Chemical Biology Molecular Modeling Therapeutics Enzyme Inhibition Natural Products Medicinal Chemistry
Areas of Focus
  • Medicinal Chemistry
  • Organic Chemistry
Work Experience
  • 2018-10~Present - Chinese Academy of Sciences Shanghai Institute of Materia Medica - Researcher
  • 2012-11~2018-09 - Chinese Academy of Sciences Shanghai Institute of Materia Medica - Associate Researcher
  • 2012-07~2012-10 - Chinese Academy of Sciences Shanghai Institute of Materia Medica - Assistant Researcher
  • 2010-06~2012-06 - Chinese Academy of Sciences Shanghai Institute of Materia Medica - Postdoctoral Researcher
Academic Background & Achievements
  • 2005-09--2010-03 PhD: East China University of Science and Technology
Publications
  • Asymmetric macrocyclization enabled by Rh(III)-catalyzed C-H activation: Enantioenriched macrocyclic inhibitor of Zika virus infection, Chinese Chemical Letters, 2024
  • Discovery of Highly Potent and Selective Thyroid Hormone Receptor Agonists for the Treatment of Nonalcoholic Steatohepatitis, Journal of Medicinal Chemistry, 2023
  • Cyclization strategy leads to highly potent Bromodomain and extra-terminal (BET) Bromodomain inhibitors for the treatment of acute liver injury, European Journal of Medicinal Chemistry, 2023
  • Rh(III)-catalyzed twofold unsymmetrical C-H alkenylation-annulation/amidation reaction enabled delivery of diverse furoquinazolinones, TETRAHEDRON LETTERS, 2022
  • Ruthenium(II)-Catalyzed ortho Hydroxymethylation of 6-Arylpurines with Paraformaldehyde via Purine-Directed C-H Activation, Heterocycles, 2022
  • Discovery of a Potent and Selective Degrader for USP7, ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2022
  • Rhodium(III)-Catalyzed Asymmetric 1,2-Carboamidation of Alkenes Enables Access to Chiral 2,3-Dihydro-3-benzofuranmethanamides, ORGANIC LETTERS, 2022
  • Discovery of novel Thieno2,3-dimidazole derivatives as agonists of human STING for antitumor immunotherapy using systemic administration, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2022
  • Rh(III)-catalyzed selective C7-H functionalization of indolines with 1,3-enynes enables access to six-membered 1,7-fused indolines, TETRAHEDRON LETTERS, 2021
  • Rhodium-Catalyzed Twofold Unsymmetrical C-H Alkenylation-Annulation/Thiolation Reaction To Access Thiobenzofurans, ORGANIC LETTERS, 2021
  • Discovery of thalidomide-based PROTAC small molecules as the highly efficient SHP2 degraders, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021
  • Design, synthesis and biological evaluation of a novel spiro oxazolidinedione as potent p300/CBP HAT inhibitor for the treatment of ovarian cancer, BIOORGANIC & MEDICINAL CHEMISTRY, 2021
  • P300/CBP inhibition sensitizes mantle cell lymphoma to PI3K delta inhibitor idelalisib, ACTA PHARMACOLOGICA SINICA, 2021
  • Recent advances of pharmacological activities and structural modifications of celastrol, 中国药物化学杂志, 2020
  • Rh(iii)-catalyzed tandem annulative redox-neutral arylation/amidation of aromatic tethered alkenes, CHEMICAL SCIENCE, 2020
  • Discovery of 8-Methyl-pyrrolo1,2-apyrazin-1(2H)-one Derivatives as Highly Potent and Selective Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitors, JOURNAL OF MEDICINAL CHEMISTRY, 2020
  • RUTHENIUM(II)-CATALYZED REGIOSELECTIVE C-H HYDROXYMETHYLATION OF N-ARYL-AZAINDOLES WITH PARAFORMALDEHYDE, HETEROCYCLES, 2020
  • Discovery of Highly Potent, Selective, and Orally Efficacious p300/CBP Histone Acetyltransferases Inhibitors, JOURNAL OF MEDICINAL CHEMISTRY, 2020
  • Ruthenium(II)-Catalyzed Regioselective Ortho C-H Allenylation of Electron-Rich Aniline and Phenol Derivatives, JOURNAL OF ORGANIC CHEMISTRY, 2020
  • Ru(II)-catalyzed regioselective C-7 hydroxymethylation of indolines with formaldehyde, TETRAHEDRON LETTERS, 2019
  • Discovery and biological evaluation of vinylsulfonamide derivatives as highly potent, covalent TEAD autopalmitoylation inhibitors, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2019
  • p300/CBP inhibitor A-485 alleviates acute liver injury by regulating macrophage activation and polarization, THERANOSTICS, 2019
  • Rh(III)-Catalyzed Redox-Neutral Unsymmetrical C-H Alkylation and Amidation Reactions of &ITN&IT-Phenoxyacetamides, JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2018
  • Experimental and theoretical studies on rhodium-catalyzed direct CsbndH benzoxylation reaction, TETRAHEDRON LETTERS, 2018
  • Rhodium-Catalyzed C-H Functionalization of Indoles with Diazo Compounds: Synthesis of Structurally Diverse 2,3-Fused Indoles, ADVANCEDSYNTHESISCATALYSIS, 2018
  • A Rh(III)-catalyzed redox-neutral C-H alkylation reaction with allylic alcohols by using a traceless oxidizing directing group, ORGANIC CHEMISTRY FRONTIERS, 2018
  • Discovery and biological evaluation of thiobarbituric derivatives as potent p300/CBP inhibitors, BIOORGANIC & MEDICINAL CHEMISTRY, 2018
  • Experimental and theoretical studies on rhodium-catalyzed direct C-H benzoxylation reaction, TETRAHEDRON LETTERS, 2018
  • Discovery and optimization of selective inhibitors of protein arginine methyltransferase 5 by docking-based virtual screening, ORGANIC & BIOMOLECULAR CHEMISTRY, 2017
  • Rhodium(iii)-catalyzed alkylation of primary C(sp(3))-H bonds with ��-diazocarbonyl compounds., 2016-01-01
  • 去氢表雄酮衍生物的合成及其抑制神经炎症活性研究, 中国药物化学杂志, 2016
  • Rhodium(iii)-catalyzed alkyllation of primary c(sp(3))-h bonds with alpha-diazocarbonyl compounds, CHEMICAL COMMUNICATIONS, 2016
  • Identification of novel small-molecule inhibitors targeting menin-MLL interaction, repurposing the antidiarrheals loperamide, Org. Biomol. Chem., 2016
  • Identification of novel small-molecule inhibitors targeting menin-MLL interaction, repurposing the antidiarrheal loperamide, ORGANIC & BIOMOLECULAR CHEMISTRY, 2016
  • Chiral discrimination of natural isoflavanones using (R)- and (S)-BINOL as the NMR chiral solvating agents, TETRAHEDRON-ASYMMETRY, 2016
  • Redox-Neutral Rhodium-Catalyzed C-H Functionalization of Arylamine N-Oxides with Diazo Compounds: Primary C(sp(3))-H/C(sp(2))-H Activation and Oxygen-Atom Transfer, ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2015
  • Ir-III-Catalyzed Direct C-7 Amidation of Indolines with Sulfonyl, Acyl, and Aryl Azides at Room Temperature, EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, 2015
  • Iridium(III)-Catalyzed C-7 Selective C-H Alkynylation of Indolines at Room Temperature, JOURNAL OF ORGANIC CHEMISTRY, 2015
  • Rh(III)- or Ir(III)-catalyzed ynone synthesis from aldehydes via chelation-assisted C-H bond activation, CHEMICAL COMMUNICATIONS, 2015
  • A 4+1 Cyclative Capture Approach to 3H-Indole-N-oxides at Room Temperature by Rhodium(III)-Catalyzed C-H Activation, ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2015
  • Rhodium-Catalyzed Redox-Neutral C-H Functionalization of Arylamine N-Oxides with Diazo Compounds: Primary C(sp3)-H/C(sp2)-H Activation and Oxygen Atom Transfer., Angew.Chem. Int. Ed., 2015
  • Access to Six- and Seven-Membered 1,7-Fused Indolines via Rh(III)-Catalyzed Redox-Neutral C7-Selective C-H Functionalization of Indolines with Alkynes and Alkenes, JOURNAL OF ORGANIC CHEMISTRY, 2015
Awards
  • Chinese Academy of Sciences Youth Innovation Promotion Association Member (2017): Other
  • Sanofi-Aventis - Chinese Academy of Sciences Shanghai Institute of Life Sciences Outstanding Young Talent Award (2016): Other
  • Synthesis of an important intermediate of the new class 1 drug 'Letenshu' (LLDT-8) (2012): Second Prize, Municipal Level
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