PMID

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Article Title

Organization

Novel 3-methylindoline inhibitors of EZH2: Design, synthesis and SAR.

Integral Biosciences

Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.

Pfizer

Identification of novel EZH2 inhibitors through pharmacophore-based virtual screening and biological assays.

College of Chemical and Environmental Engineering

The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat.

Epizyme

Discovery, design, and synthesis of indole-based EZH2 inhibitors.

Constellation Pharmaceuticals

Selective inhibitors of protein methyltransferases.

Icahn School of Medicine At Mount Sinai

SAH derived potent and selective EZH2 inhibitors.

Pfizer

The role of enhancer of zeste homologue 2 inhibitors in controlling epigenetics and their potential for cancer treatment.

Therachem Research Medilab (India)

Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2.

Constellation Pharmaceuticals

Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.

TBA

Quinoline anticancer agents active on DNA and DNA-interacting proteins: From classical to emerging therapeutic targets.

University of Palermo

Blocking Non-enzymatic Functions by PROTAC-Mediated Targeted Protein Degradation.

Second Military Medical University (Naval Medical University)

Focused Libraries for Epigenetic Drug Discovery: The Importance of Isosteres.

University of Pennsylvania

Recent advances in epigenetic proteolysis targeting chimeras (Epi-PROTACs).

"Sapienza" University of Rome

Targeting Autophagy-Related Epigenetic Regulators for Cancer Drug Discovery.

West China Hospital of Sichuan University

Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.

Menoufia University

Structure-Aided Design, Synthesis, and Biological Evaluation of Potent and Selective Non-Nucleoside Inhibitors Targeting Protein Arginine Methyltransferase 5.

Sun Yat-Sen University

Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors.

Sun Yat-Sen University Cancer Center

Fascinating Transformation of SAM-Competitive Protein Methyltransferase Inhibitors from Nucleoside Analogues to Non-Nucleoside Analogues.

Csir-Indian Institute of Chemical Biology

Novel Quinoline Compounds as EZH2 Inhibitors for Treating Cancer.

Smith, Gambrell & Russell

Recent strategies targeting Embryonic Ectoderm Development (EED) for cancer therapy: Allosteric inhibitors, PPI inhibitors, and PROTACs.

Sanquan College of Xinxiang Medical University

Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects.

Affiliated Hospital of Guangdong Medical University

Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models.

Sapienza University of Rome

Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.

Indian Institute of Technology (B.H.U.)

Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.

China Pharmaceutical University

Targeting EZH2 for cancer therapy: From current progress to novel strategies.

West China Hospital

A Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors.

Tri-Institutional Therapeutics Discovery Institute

Design and Synthesis of EZH2-Based PROTACs to Degrade the PRC2 Complex for Targeting the Noncatalytic Activity of EZH2.

Sichuan University

Discovery of

China Pharmaceutical University

Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.

Chinese Academy of Sciences

Discovery of First-in-Class Dual PARP and EZH2 Inhibitors for Triple-Negative Breast Cancer with Wild-Type BRCA.

China Pharmaceutical University

Discovery of a potent MLL1 and WDR5 protein-protein interaction inhibitor with in vivo antitumor activity.

China Pharmaceutical University

5-Aminonaphthalene derivatives as selective nonnucleoside nuclear receptor binding SET domain-protein 2 (NSD2) inhibitors for the treatment of multiple myeloma.

Chinese Academy of Sciences

Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymp

Constellation Pharmaceuticals

Design and Characterization of a Pyridone-Containing EZH2 Inhibitor Phosphate Prodrug.

TBA

Small Molecule Approaches for Targeting the Polycomb Repressive Complex 2 (PRC2) in Cancer.

Northwestern University

Identification of DOT1L inhibitors by structure-based virtual screening adapted from a nucleoside-focused library.

University of Michigan Medical School

Monomeric Targeted Protein Degraders.

TBA

Design and synthesis of (E)-1,2-diphenylethene-based EZH2 inhibitors.

Sichuan University and Collaborative Innovation Center

Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time.

Constellation Pharmaceuticals

Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.

Sapienza University of Rome

New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms.

University College London

Structure-Activity Relationship Studies for Enhancer of Zeste Homologue 2 (EZH2) and Enhancer of Zeste Homologue 1 (EZH1) Inhibitors.

Icahn School of Medicine At Mount Sinai

Histone methyl transferases: A class of epigenetic opportunities to counter uncontrolled cell proliferation.

Punjabi University

Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma.

Shanghai Hengrui Pharmaceutical

Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquin

Wuxi Apptec