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[ASAP] Multicomponent Microscale Biosynthesis of Unnatural Cyanobacterial Indole Alkaloids

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Published On :: Thu, 07 May 2020 04:00:00 GMT

ACS Synthetic Biology

DOI: 10.1021/acssynbio.0c00038

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Dads, What Is the Culture of the Home You Are Building?

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It doesn’t require status or wealth to be a good dad, just trust in following God.

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[ASAP] MymA Bioactivated Thioalkylbenzoxazole Prodrug Family Active against <italic toggle="yes">Mycobacterium tuberculosis</italic>

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Published On :: Sun, 19 Apr 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.0c00003

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[ASAP] A Selective Modulator of Peroxisome Proliferator-Activated Receptor ? with an Unprecedented Binding Mode

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Published On :: Mon, 20 Apr 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.9b01786

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[ASAP] Imidazo[1,2-<italic toggle="yes">a</italic>]pyridine Derivatives as Aldehyde Dehydrogenase Inhibitors: Novel Chemotypes to Target Glioblastoma Stem Cells

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Published On :: Mon, 20 Apr 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.9b01910

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[ASAP] Synthesis and Structure–Activity Relationships of Arylsulfonamides as AIMP2-DX2 Inhibitors for the Development of a Novel Anticancer Therapy

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Published On :: Tue, 21 Apr 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.9b01961

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[ASAP] Discovery, Structure–Activity Relationship, and Biological Activity of Histone-Competitive Inhibitors of Histone Acetyltransferases P300/CBP

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Published On :: Tue, 21 Apr 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.9b02164

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[ASAP] Metabolism and Bioactivation: It’s Time to Expect the Unexpected<subtitle>Miniperspective</subtitle>

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Published On :: Tue, 21 Apr 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.0c00026

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[ASAP] Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation

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Published On :: Wed, 22 Apr 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.0c00035

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[ASAP] Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands

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Published On :: Thu, 23 Apr 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.9b01835

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[ASAP] Update to Our Reader, Reviewer, and Author Communities—April 2020

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Published On :: Thu, 23 Apr 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.0c00641

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[ASAP] Discovery of Peptide Boronate Derivatives as Histone Deacetylase and Proteasome Dual Inhibitors for Overcoming Bortezomib Resistance of Multiple Myeloma

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Published On :: Thu, 23 Apr 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.9b02161

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[ASAP] Correction to Toggling Preassembly with Single-Site Mutation Switches the Cytotoxic Mechanism of Cationic Amphipathic Peptides

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Published On :: Fri, 24 Apr 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.0c00608

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[ASAP] Positional Analogue Scanning: An Effective Strategy for Multiparameter Optimization in Drug Design

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Published On :: Fri, 24 Apr 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.9b02092

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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

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Published On :: Mon, 27 Apr 2020 04:00:00 GMT

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

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Published On :: Mon, 27 Apr 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.9b02097

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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

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Published On :: Mon, 27 Apr 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.9b02035

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

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Published On :: Mon, 27 Apr 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.0c00161

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[ASAP] Correction to Photoactivatable Prolyl Hydroxylase 2 Inhibitors for Stabilizing the Hypoxia-Inducible Factor with Light

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Published On :: Tue, 28 Apr 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.0c00599

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

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Published On :: Tue, 28 Apr 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.9b01336

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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

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Published On :: Wed, 29 Apr 2020 04:00:00 GMT

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

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Published On :: Thu, 30 Apr 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.0c00101

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[ASAP] Computational Chemistry on a Budget: Supporting Drug Discovery with Limited Resources<subtitle>Miniperspective</subtitle>

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Published On :: Fri, 01 May 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.9b02126

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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

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Published On :: Mon, 04 May 2020 04:00:00 GMT

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

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Published On :: Tue, 05 May 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.0c00395

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[ASAP] p62/SQSTM1, a Central but Unexploited Target: Advances in Its Physiological/Pathogenic Functions and Small Molecular Modulators

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Published On :: Tue, 05 May 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.9b02038

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[ASAP] Both <sc>d</sc>- and <sc>l</sc>-Glucose Polyphosphates Mimic <sc>d</sc>-<italic toggle="yes">myo</italic>-Inositol 1,4,5-Trisphosphate: New Synthetic Agonists and Partial Agonists at the Ins

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Published On :: Wed, 06 May 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.0c00215

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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

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Published On :: Wed, 06 May 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.0c00231

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

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Published On :: Wed, 06 May 2020 04:00:00 GMT

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

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Published On :: Wed, 06 May 2020 04:00:00 GMT

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

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Published On :: Thu, 07 May 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.0c00337

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

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Published On :: Thu, 07 May 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.0c00082

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[ASAP] Ruthenium(II) Complex Containing a Redox-Active Semiquinonate Ligand as a Potential Chemotherapeutic Agent: From Synthesis to <italic toggle="yes">In Vivo</italic> Studies

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Published On :: Thu, 07 May 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.0c00431

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

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Published On :: Fri, 08 May 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.0c00153

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[ASAP] Discovery and Optimization of Glucose Uptake Inhibitors

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Published On :: Fri, 08 May 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.9b02153

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[ASAP] Molecular Basis for Omapatrilat and Sampatrilat Binding to Neprilysin—Implications for Dual Inhibitor Design with Angiotensin-Converting Enzyme

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Published On :: Fri, 08 May 2020 04:00:00 GMT

Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.0c00441

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

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Published On :: Mon, 30 Mar 2020 04:00:00 GMT

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

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Published On :: Mon, 30 Mar 2020 04:00:00 GMT

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

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Published On :: Mon, 30 Mar 2020 04:00:00 GMT

ACS Medicinal Chemistry Letters

DOI: 10.1021/acsmedchemlett.9b00664

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

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Published On :: Wed, 01 Apr 2020 04:00:00 GMT

ACS Medicinal Chemistry Letters

DOI: 10.1021/acsmedchemlett.0c00116

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

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Published On :: Thu, 02 Apr 2020 04:00:00 GMT

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

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Published On :: Thu, 02 Apr 2020 04:00:00 GMT

ACS Medicinal Chemistry Letters

DOI: 10.1021/acsmedchemlett.0c00045

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[ASAP] Escaping from Flatland: Substituted Bridged Pyrrolidine Fragments with Inherent Three-Dimensional Character

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Published On :: Thu, 02 Apr 2020 04:00:00 GMT

ACS Medicinal Chemistry Letters

DOI: 10.1021/acsmedchemlett.0c00039

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

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Published On :: Fri, 03 Apr 2020 04:00:00 GMT

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

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Published On :: Mon, 06 Apr 2020 04:00:00 GMT

ACS Medicinal Chemistry Letters

DOI: 10.1021/acsmedchemlett.9b00526

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[ASAP] Rationally Designed Covalent BCL6 Inhibitor That Targets a Tyrosine Residue in the Homodimer Interface

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Published On :: Tue, 07 Apr 2020 04:00:00 GMT

ACS Medicinal Chemistry Letters

DOI: 10.1021/acsmedchemlett.0c00111

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

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Published On :: Wed, 08 Apr 2020 04:00:00 GMT

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

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Published On :: Wed, 08 Apr 2020 04:00:00 GMT

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

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Published On :: Thu, 09 Apr 2020 04:00:00 GMT

ACS Medicinal Chemistry Letters

DOI: 10.1021/acsmedchemlett.9b00681

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

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Published On :: Fri, 10 Apr 2020 04:00:00 GMT

ACS Medicinal Chemistry Letters

DOI: 10.1021/acsmedchemlett.9b00574