Journal of Medicinal Chemistry

[ASAP] Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression (Mon, 10 Dec 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00909

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[ASAP] Novel Tetrazole-Containing Analogues of Itraconazole as Potent Antiangiogenic Agents with Reduced Cytochrome P450 3A4 Inhibition (Mon, 10 Dec 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01252

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[ASAP] Aliphatic Azides as Selective Cysteine Labeling Reagents for Integral Membrane Proteins (Mon, 10 Dec 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01302

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[ASAP] Identification of 5-(2,3-Dihydro-1<italic toggle="yes">H</italic>-indol-5-yl)-7<italic toggle="yes">H</italic>-pyrrolo[2,3-<italic toggle="yes">d</italic>]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model (Mon, 10 Dec 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01652

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[ASAP] Celastrol Promotes Weight Loss in Diet-Induced Obesity by Inhibiting the Protein Tyrosine Phosphatases PTP1B and TCPTP in the Hypothalamus (Fri, 07 Dec 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01224

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[ASAP] Correction to Optimization of 1,4-Oxazine ß-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate (Fri, 07 Dec 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01859

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[ASAP] Structural and Functional Assessment of mBjAMP1, an Antimicrobial Peptide from <italic toggle="yes">Branchiostoma japonicum</italic>, Revealed a Novel a-Hairpinin-like Scaffold with Membrane Permeable and DNA Binding Activity (Thu, 06 Dec 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01135

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[ASAP] <italic toggle="yes">qFit-ligand</italic> Reveals Widespread Conformational Heterogeneity of Drug-Like Molecules in X-Ray Electron Density Maps (Thu, 06 Dec 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01292

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[ASAP] Small Molecule Inhibitor that Stabilizes the Autoinhibited Conformation of the Oncogenic Tyrosine Phosphatase SHP2 (Wed, 05 Dec 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00513

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[ASAP] Selective Inhibitors of Human Neuraminidase 1 (NEU1) (Wed, 05 Dec 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01411

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[ASAP] Semisynthesis of Platensimycin Derivatives with Antibiotic Activities in Mice via Suzuki–Miyaura Cross-Coupling Reactions (Wed, 05 Dec 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01580

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[ASAP] Structure–Activity Relationships of Photoswitchable Diarylethene-Based ß-Hairpin Peptides as Membranolytic Antimicrobial and Anticancer Agents (Tue, 04 Dec 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01428

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[ASAP] Bisphosphonate Inhibitors of Mammalian Glycolytic Aldolase (Mon, 03 Dec 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01000

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[ASAP] Polyheteroaryl Oxazole/Pyridine-Based Compounds Selected in Vitro as G-Quadruplex Ligands Inhibit Rock Kinase and Exhibit Antiproliferative Activity (Mon, 03 Dec 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01023

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[ASAP] Proline- and Arginine-Rich Peptides as Flexible Allosteric Modulators of Human Proteasome Activity (Mon, 03 Dec 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01025

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[ASAP] Design, Synthesis, and Antifibrosis Activity in Liver of Nonsecosteroidal Vitamin D Receptor Agonists with Phenyl-pyrrolyl Pentane Skeleton (Mon, 03 Dec 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01165

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[ASAP] A Drug with Lipophilicity-Dependent Potency Can Be Metabolically Stable: Discovery of a Potent and Selective Retinoic Acid Receptor-Related Orphan Receptor C2 (RORC2) Inverse Agonist as an Orally Bioavailable Anti-Inflammatory Agent (Mon, 03 Dec 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01545

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[ASAP] The Chimera That Curbs Appetite (Mon, 03 Dec 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01809

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[ASAP] Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors (Fri, 30 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01308

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[ASAP] Amyloid-Binding Alcohol Dehydrogenase (ABAD) Inhibitors for the Treatment of Alzheimer’s Disease<subtitle>Miniperspective</subtitle> (Fri, 30 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01530

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[ASAP] A Survey of the Structures of US FDA Approved Combination Drugs (Fri, 30 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01610

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[ASAP] Computational Method to Evaluate Progress in Lead Optimization (Fri, 30 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01626

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[ASAP] Sterol 14a-Demethylase Structure-Based Optimization of Drug Candidates for Human Infections with the Protozoan Trypanosomatidae (Fri, 30 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01671

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[ASAP] Discovery of Clinical Candidate 2-(4-(2-((1<italic toggle="yes">H</italic>-Benzo[<italic toggle="yes">d</italic>]imidazol-2-yl)thio)ethyl)piperazin-1-yl)-<italic toggle="yes">N</italic>-(6-methyl-2,4-bis(methylthio)pyridin-3-yl)acetamide Hydrochloride [K-604], an Aqueous-Soluble Acyl-CoA:Cholesterol <italic toggle="yes">O</italic>-Acyltransferase-1 Inhibitor (Thu, 29 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01256

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[ASAP] Synthesis and Discovery Novel Anti-Cancer Stem Cells Compounds Derived from the Natural Triterpenoic Acids (Thu, 29 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01445

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[ASAP] Novel Symmetrical Benzazolyl Derivatives Endowed with Potent Anti-Heparanase Activity (Thu, 29 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01497

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[ASAP] Optimization of Novel 1-Methyl-1<italic toggle="yes">H</italic>-Pyrazole-5-carboxamides Leads to High Potency Larval Development Inhibitors of the Barber’s Pole Worm (Thu, 29 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01544

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[ASAP] Neolymphostin A Is a Covalent Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitor That Employs an Unusual Electrophilic Vinylogous Ester (Wed, 28 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00975

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[ASAP] Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Inhibition: An Emerging Strategy in Cancer Therapy (Wed, 28 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01121

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[ASAP] Reducing the Lipophilicity of Perfluoroalkyl Groups by CF2–F/CF2–Me or CF3/CH3 Exchange (Wed, 28 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01222

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[ASAP] 4-Hydroxy-3-nitro-5-ureido-benzenesulfonamides Selectively Target the Tumor-Associated Carbonic Anhydrase Isoforms IX and XII Showing Hypoxia-Enhanced Antiproliferative Profiles (Wed, 28 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01504

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[ASAP] Aminergic GPCR–Ligand Interactions: A Chemical and Structural Map of Receptor Mutation Data (Tue, 27 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00836

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[ASAP] Noncovalent Inhibitors of Mosquito Acetylcholinesterase 1 with Resistance-Breaking Potency (Tue, 27 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01060

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[ASAP] Functional Characterization of a Novel Lipopolysaccharide-Binding Antimicrobial and Anti-Inflammatory Peptide in Vitro and in Vivo (Tue, 27 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01358

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[ASAP] Highly Potent 17ß-HSD2 Inhibitors with a Promising Pharmacokinetic Profile for Targeted Osteoporosis Therapy (Tue, 27 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01373

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[ASAP] Design, Synthesis, and Biological Evaluation of Cytochrome P450 1B1 Targeted Molecular Imaging Probes for Colorectal Tumor Detection (Tue, 27 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01633

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[ASAP] Potent Antiglioblastoma Agents by Hybridizing the Onium-Alkyloxy-Stilbene Based Structures of an a7-nAChR, a9-nAChR Antagonist and of a Pro-Oxidant Mitocan (Mon, 26 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01052

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[ASAP] Structure-Based Approach toward Identification of Inhibitory Fragments for Eleven-Nineteen-Leukemia Protein (ENL) (Mon, 26 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01457

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[ASAP] Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[<italic toggle="yes">c</italic>]pyrrolo[2,3-<italic toggle="yes">h</italic>][1,6]naphthyridin-5-one (BPN) Series (Wed, 21 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00510

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[ASAP] Battle against Vancomycin-Resistant Bacteria: Recent Developments in Chemical Strategies (Wed, 21 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01093

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[ASAP] State of the Art in Respiratory Syncytial Virus Drug Discovery and Development (Wed, 21 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01361

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[ASAP] Fragment-to-Lead Medicinal Chemistry Publications in 2017<subtitle>Miniperspective</subtitle> (Wed, 21 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01472

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[ASAP] Design of Y2 Receptor Selective and Proteolytically Stable PYY3–36 Analogues (Tue, 20 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01046

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[ASAP] Pyridinium Oximes with <italic toggle="yes">Ortho</italic>-Positioned Chlorine Moiety Exhibit Improved Physicochemical Properties and Efficient Reactivation of Human Acetylcholinesterase Inhibited by Several Nerve Agents (Tue, 20 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01398

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[ASAP] Tanshinone-IIA-Based Analogues of Imidazole Alkaloid Act as Potent Inhibitors To Block Breast Cancer Invasion and Metastasis in Vivo (Mon, 19 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01018

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[ASAP] Cell-Active Small Molecule Inhibitors of the DNA-Damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides (Mon, 19 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01407

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[ASAP] Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy (Fri, 16 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00189

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[ASAP] Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects<subtitle>Miniperspective</subtitle> (Fri, 16 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01531

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[ASAP] Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A (Thu, 15 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01219

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[ASAP] Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of <italic toggle="yes">Staphylococcus aureus</italic> (Thu, 15 Nov 2018)

Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01293

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