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[ASAP] Discovery and Development of S6821 and S7958 as Potent TAS2R8 Antagonists

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00388




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[ASAP] Discovery and Structure–Activity Relationship Study of (<italic toggle="yes">Z</italic>)-5-Methylenethiazolidin-4-one Derivatives as Potent and Selective Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00227




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[ASAP] Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b02097




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[ASAP] Discovery of M-808 as a Highly Potent, Covalent, Small-Molecule Inhibitor of the Menin–MLL Interaction with Strong <italic toggle="yes">In Vivo</italic> Antitumor Activity

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00547




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[ASAP] Treating Cancer by Spindle Assembly Checkpoint Abrogation: Discovery of Two Clinical Candidates, BAY 1161909 and BAY 1217389, Targeting MPS1 Kinase

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b02035




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[ASAP] Structure–Activity Relationship of SPOP Inhibitors against Kidney Cancer

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00161




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[ASAP] Discovery of (2<italic toggle="yes">R</italic>)-<italic toggle="yes">N</italic>-[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1<italic toggle="yes">H</italic>-indol-7

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01392




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[ASAP] Bioisosteric Discovery of NPA101.3, a Second-Generation RET/VEGFR2 Inhibitor Optimized for Single-Agent Polypharmacology

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01336




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[ASAP] Structure-Based Design of Highly Potent HIV-1 Protease Inhibitors Containing New Tricyclic Ring P2-Ligands: Design, Synthesis, Biological, and X-ray Structural Studies

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00202




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[ASAP] Design, Synthesis, and Mechanism Study of Benzenesulfonamide-Containing Phenylalanine Derivatives as Novel HIV-1 Capsid Inhibitors with Improved Antiviral Activities

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00015




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[ASAP] Design and Characterization of the First Selective and Potent Mechanism-Based Inhibitor of Cytochrome P450 4Z1

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00101




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[ASAP] Design of Radiolabeled Analogs of Minigastrin by Multiple Amide-to-Triazole Substitutions

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b01937




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[ASAP] Degradation versus Inhibition: Development of Proteolysis-Targeting Chimeras for Overcoming Statin-Induced Compensatory Upregulation of 3-Hydroxy-3-methylglutaryl Coenzyme A Reductase

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00339




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[ASAP] Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00395




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[ASAP] Structural Fingerprints of an Intact Monoclonal Antibody Acquired under Formulated Storage Conditions via <sup>15</sup>N Direct Detection Nuclear Magnetic Resonance

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00231




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[ASAP] Discovery of Potent, Selective, and Orally Bioavailable Inhibitors of USP7 with In Vivo Antitumor Activity

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00245




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[ASAP] Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00021




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[ASAP] Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00442




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[ASAP] Discovery of Potent Inhibitors against P-Glycoprotein-Mediated Multidrug Resistance Aided by Late-Stage Functionalization of a 2-(4-(Pyridin-2-yl)phenoxy)pyridine Analogue

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00337




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[ASAP] Discovery of <italic toggle="yes">N</italic>-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1<italic toggle="yes">H</italic>-pyrrolo[2,3-<italic toggle=&q

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00628




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[ASAP] Discovery of a Silicon-Containing Pan-Genotype Hepatitis C Virus NS5A Inhibitor

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00082




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[ASAP] Exploration of the Structural Space in 4(3<italic toggle="yes">H</italic>)-Quinazolinone Antibacterials

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c00153




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[ASAP] Discovery and Optimization of Glucose Uptake Inhibitors

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.9b02153




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[ASAP] Discovery of a Cyclic Choline Analog That Inhibits Anaerobic Choline Metabolism by Human Gut Bacteria

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.0c00005




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[ASAP] Discovery of Selective, Covalent FGFR4 Inhibitors with Antitumor Activity in Models of Hepatocellular Carcinoma

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.9b00601




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[ASAP] Chimeric Peptidomimetics of SOCS 3 Able to Interact with JAK2 as Anti-inflammatory Compounds

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.9b00664




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[ASAP] Progress in the Field of Aldehyde Dehydrogenase Inhibitors: Novel Imidazo[1,2-<italic toggle="yes">a</italic>]pyridines against the 1A Family

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.9b00686




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[ASAP] Cancer Immunotherapy through the Inhibition of Diacylglycerol Kinases Alpha and Zeta

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.0c00118




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[ASAP] Inhibitors of Hypoxia-Inducible Factors as Treatment for Cancer

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.0c00116




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[ASAP] Glycans Meet Sphingolipids: Structure-Based Design of Glycan Containing Analogues of a Sphingosine Kinase Inhibitor

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.9b00665




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[ASAP] Therapeutic Potential of Targeted Nanoparticles and Perspective on Nanotherapies

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.0c00075




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[ASAP] Synthesis of Novel G Factor or Chloroquine-Artemisinin Hybrids and Conjugates with Potent Antiplasmodial Activity

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.9b00669




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[ASAP] Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.0c00045




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[ASAP] Characterization of an Alginate Encapsulated LS180 Spheroid Model for Anti-colorectal Cancer Compound Screening

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.0c00076




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[ASAP] Structure Optimization of Gatastatin for the Development of ?-Tubulin-Specific Inhibitor

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.9b00526




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[ASAP] Chiral Analogues of PFI-1 as BET Inhibitors and Their Functional Role in Myeloid Malignancies

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.9b00625




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[ASAP] Assembling Pharma Resources to Tackle Diseases of Underserved Populations

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.0c00051




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[ASAP] Pharmacophore-Based Virtual Screening for Identification of Negative Modulators of GLI1 as Potential Anticancer Agents

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.9b00639




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[ASAP] Exploring the Implication of DDX3X in DENV Infection: Discovery of the First-in-Class DDX3X Fluorescent Inhibitor

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.9b00681




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[ASAP] Discovery of BMS-986251: A Clinically Viable, Potent, and Selective ROR?t Inverse Agonist

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.0c00063




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[ASAP] Combined Peptide and Small-Molecule Approach toward Nonacidic THIQ Inhibitors of the KEAP1/NRF2 Interaction

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.9b00594




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[ASAP] Selective Covalent Targeting of Mutated EGFR(T790M) with Chlorofluoroacetamide-Pyrimidines

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.9b00574




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[ASAP] Design and Synthesis of Tetrazole- and Pyridine-Containing Itraconazole Analogs as Potent Angiogenesis Inhibitors

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.9b00438




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[ASAP] Potential Cancer Treatment by Agonists of the Stimulator of Interferon Genes

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.0c00117




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[ASAP] Complete Regression of Carcinoma via Combined C-RAF and EGFR Targeted Therapy

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.0c00159




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[ASAP] Discovery of a Potent Dual Inhibitor of Wild-Type and Mutant Respiratory Syncytial Virus Fusion Proteins

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.0c00008




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[ASAP] Characterization of Specific <italic toggle="yes">N</italic>-a-Acetyltransferase 50 (Naa50) Inhibitors Identified Using a DNA Encoded Library

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.0c00029




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[ASAP] Discovery of an Atropisomeric PI3Kß Selective Inhibitor through Optimization of the Hinge Binding Motif

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.0c00095




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[ASAP] Discovery of CPI-1612: A Potent, Selective, and Orally Bioavailable EP300/CBP Histone Acetyltransferase Inhibitor

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.0c00155




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[ASAP] Development of Selective Steroid Inhibitors for the Glucose-6-phosphate Dehydrogenase from <italic toggle="yes">Trypanosoma cruzi</italic>

ACS Medicinal Chemistry Letters
DOI: 10.1021/acsmedchemlett.0c00106