Journal of Medicinal Chemistry

Glycosylated Platinum(IV) Complexes as Substrates for Glucose Transporters (GLUTs) and Organic Cation Transporters (OCTs) Exhibited Cancer Targeting and Human Serum Albumin Binding Properties for Drug Delivery (Tue, 27 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00433
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Synthesis and Preclinical Characterization of a Cationic Iodinated Imaging Contrast Agent (CA4+) and Its Use for Quantitative Computed Tomography of Ex Vivo Human Hip Cartilage (Tue, 27 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00234
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Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines (Tue, 27 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00137
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In Vivo and Mechanistic Studies on Antitumor Lead 7-Methoxy-4-(2-methylquinazolin-4-yl)-3,4-dihydroquinoxalin-2(1H)-one and Its Modification as a Novel Class of Tubulin-Binding Tumor-Vascular Disrupting Agents (Tue, 27 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00273
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Pharmacophore Identification and Scaffold Exploration to Discover Novel, Potent, and Chemically Stable Inhibitors of Acid Ceramidase in Melanoma Cells (Tue, 27 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00472
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In Silico Absorption, Distribution, Metabolism, Excretion, and Pharmacokinetics (ADME-PK): Utility and Best Practices. An Industry Perspective from the International Consortium for Innovation through Quality in Pharmaceutical Development (Tue, 27 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00487
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Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases (Tue, 27 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01647
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Glucuronides as Potential Anionic Substrates of Human Cytochrome P450 2C8 (CYP2C8) (Tue, 27 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00510
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Correction to When Does Chemical Elaboration Induce a Ligand To Change Its Binding Mode? (Tue, 27 Jun 2017)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00868
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Structure-Based Design and Synthesis of Potent and Selective Matrix Metalloproteinase 13 Inhibitors (Tue, 27 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00514
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The Structure–Activity Relationship of a Tetrahydroisoquinoline Class of N-Methyl-d-Aspartate Receptor Modulators that Potentiates GluN2B-Containing N-Methyl-d-Aspartate Receptors (Mon, 26 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00239
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2′-Chloro,2′-fluoro Ribonucleotide Prodrugs with Potent Pan-genotypic Activity against Hepatitis C Virus Replication in Culture (Mon, 26 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00067
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1,2,4-Triazolo-[1,5-a]pyridine HIF Prolylhydroxylase Domain-1 (PHD-1) Inhibitors With a Novel Monodentate Binding Interaction (Sat, 24 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00352
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Development of Protein Degradation Inducers of Androgen Receptor by Conjugation of Androgen Receptor Ligands and Inhibitor of Apoptosis Protein Ligands (Fri, 23 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00168
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Influence of a Basic Side Chain on the Properties of Hypoxia-Selective Nitro Analogues of the Duocarmycins: Demonstration of Substantial Anticancer Activity in Combination with Irradiation or Chemotherapy (Fri, 23 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00563
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Halogen Bonding in Nucleic Acid Complexes (Fri, 23 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00329
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Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Death-Ligand 1 (PD-1/PD-L1) Interaction via Transiently Induced Protein States and Dimerization of PD-L1 (Fri, 23 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00293
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Structure-Based Optimization of Pyridoxal 5′-Phosphate-Dependent Transaminase Enzyme (BioA) Inhibitors that Target Biotin Biosynthesis in Mycobacterium tuberculosis (Fri, 23 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00189
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Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds (Fri, 23 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01912
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Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity (Thu, 22 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01755
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Paying the Price of Desolvation in Solvent-Exposed Protein Pockets: Impact of Distal Solubilizing Groups on Affinity and Binding Thermodynamics in a Series of Thermolysin Inhibitors (Thu, 22 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00490
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α-Conotoxin [S9A]TxID Potently Discriminates between α3β4 and α6/α3β4 Nicotinic Acetylcholine Receptors (Wed, 21 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00546
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Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site (Wed, 21 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00316
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Pharmaceutical Approaches to Target Antibiotic Resistance Mechanisms (Tue, 20 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00215
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Discovery of Allosteric Inhibitors Targeting the Spliceosomal RNA Helicase Brr2 (Tue, 20 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00461
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Development of 1-((1,4-trans)-4-Aryloxycyclohexyl)-3-arylurea Activators of Heme-Regulated Inhibitor as Selective Activators of the Eukaryotic Initiation Factor 2 Alpha (eIF2α) Phosphorylation Arm of the Integrated Endoplasmic Reticulum Stress Response (Mon, 19 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00059
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Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines (Mon, 19 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01538
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Compounds Interfering with Embryonic Lethal Abnormal Vision (ELAV) Protein–RNA Complexes: An Avenue for Discovering New Drugs (Mon, 19 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01871
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Hepatitis C Virus NS3/4A Protease Inhibitors Incorporating Flexible P2 Quinoxalines Target Drug Resistant Viral Variants (Mon, 19 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00426
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Insights on the Interaction between Transthyretin and Aβ in Solution. A Saturation Transfer Difference (STD) NMR Analysis of the Role of Iododiflunisal (Fri, 16 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00428
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The 1,2,4-Triazolo[4,3-a]pyrazin-3-one as a Versatile Scaffold for the Design of Potent Adenosine Human Receptor Antagonists. Structural Investigations to Target the A2A Receptor Subtype (Fri, 16 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00457
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Discovery of Novel 11-Triazole Substituted Benzofuro[3,2-b]quinolone Derivatives as c-myc G-Quadruplex Specific Stabilizers via Click Chemistry (Fri, 16 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00016
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Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor (Fri, 16 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00397
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Design, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups (Fri, 16 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00197
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Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors (Fri, 16 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00572
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Discovery of Small Molecules for Repressing Cap-Independent Translation of Human Vascular Endothelial Growth Factor (hVEGF) as Novel Antitumor Agents (Fri, 16 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01444
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Development and Characterization of a Fluorescent Tracer for the Free Fatty Acid Receptor 2 (FFA2/GPR43) (Fri, 16 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00338
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A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication (Thu, 15 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00175
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Targeting Mycolic Acid Transport by Indole-2-carboxamides for the Treatment of Mycobacterium abscessus Infections (Thu, 15 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00582
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Correction to Past, Current, and Future Developments of Therapeutic Agents for Treatment of Chronic Hepatitis B Virus Infection (Wed, 14 Jun 2017)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00781
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Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design (Wed, 14 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00231
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Phthalocyanines and Tetrapyrazinoporphyrazines with Two Cationic Donuts: High Photodynamic Activity as a Result of Rigid Spatial Arrangement of Peripheral Substituents (Wed, 14 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00272
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Chromone as a Privileged Scaffold in Drug Discovery: Recent Advances (Tue, 13 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01720
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Development of Selective Clk1 and -4 Inhibitors for Cellular Depletion of Cancer-Relevant Proteins (Wed, 31 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01915
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Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins (Wed, 24 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01817
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Unusual Undergraduate Training in Medicinal Chemistry in Collaboration between Academia and Industry (Tue, 23 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00198
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Nitric Oxide Donor-Based Cancer Therapy: Advances and Prospects (Tue, 23 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01672
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Nitroimidazoles: Molecular Fireworks That Combat a Broad Spectrum of Infectious Diseases (Mon, 22 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00143
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Targeting the Receptor for Advanced Glycation Endproducts (RAGE): A Medicinal Chemistry Perspective (Fri, 19 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00058
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Return of D4 Dopamine Receptor Antagonists in Drug Discovery (Wed, 17 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00151
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Structure-Based Design of Highly Selective Inhibitors of the CREB Binding Protein Bromodomain (Fri, 12 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01839
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Urinary Tract Infection: Which Conformation of the Bacterial Lectin FimH Is Therapeutically Relevant? (Thu, 11 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00342
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Development of a Small Hybrid Molecule That Mediates Degradation of His-Tag Fused Proteins (Wed, 10 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00413
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The Roles of Water in the Protein Matrix: A Largely Untapped Resource for Drug Discovery (Fri, 05 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00057
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Informing the Selection of Screening Hit Series with in Silico Absorption, Distribution, Metabolism, Excretion, and Toxicity Profiles (Fri, 05 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01577
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Synthetic Approaches to the New Drugs Approved During 2015 (Wed, 03 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00010
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Lead Optimization of Benzoxepin-Type Selective Estrogen Receptor (ER) Modulators and Downregulators with Subtype-Specific ERα and ERβ Activity (Mon, 01 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01917
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Past, Current, and Future Developments of Therapeutic Agents for Treatment of Chronic Hepatitis B Virus Infection (Fri, 21 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01442
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A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos (Thu, 20 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01921
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Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities (Thu, 20 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01851
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Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity (Thu, 20 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01850
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Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals) (Mon, 17 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01872
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A “Click Chemistry Platform” for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation (Mon, 17 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01781
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Protein Degradation via CRL4CRBN Ubiquitin Ligase: Discovery and Structure–Activity Relationships of Novel Glutarimide Analogs That Promote Degradation of Aiolos and/or GSPT1 (Thu, 13 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01911
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Sustainable Practices in Medicinal Chemistry Part 2: Green by Design (Wed, 12 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01837
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CNS Physicochemical Property Space Shaped by a Diverse Set of Molecules with Experimentally Determined Exposure in the Mouse Brain (Fri, 07 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01469
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Modulators of Sphingosine-1-phosphate Pathway Biology: Recent Advances of Sphingosine-1-phosphate Receptor 1 (S1P1) Agonists and Future Perspectives (Thu, 30 Mar 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01575
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Opportunities and Challenges for Fatty Acid Mimetics in Drug Discovery (Mon, 27 Mar 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01287
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Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression (Fri, 24 Mar 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01816
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Regulating the Master Regulator: Controlling Ubiquitination by Thinking Outside the Active Site (Tue, 28 Feb 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01346
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