OOIR: Observatory of International Research

Papers

(The TQCC of Journal of Medicinal Chemistry is 14. The table below lists those papers that are above that threshold based on CrossRef citation counts [max. 250 papers]. The publications cover those that have been published in the past four years, i.e., from 2021-04-01 to 2025-04-01.)

Article	Citations
Journal of Medicinal Chemistry/ACS Medicinal Chemistry Letters/Division of Medicinal Chemistry Joint Portoghese Lectureship Awards: CALL FOR NOMINATIONS	431
Discovery and Optimization of Selective Brain-Penetrant EBP Inhibitors that Enhance Oligodendrocyte Formation	402
Design, Synthesis, and Biological Evaluation of a Novel Series of 4-Guanidinobenzoate Derivatives as Enteropeptidase Inhibitors with Low Systemic Exposure for the Treatment of Obesity	369
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties	223
Issue Publication Information	218
Discovery of Potent and Selective CDK4/6 Inhibitors for the Treatment of Chemotherapy-Induced Myelosuppression	188
Issue Publication Information	178
PSMA and SSTR2 Dual-Targeting Theranostic Agents for Neuroendocrine-Differentiated Prostate Cancer (NEPC)	145
Discovery of WDR5–MLL1 and HDAC Dual-Target Inhibitors for the Treatment of Acute Myeloid Leukemia	143
Multitargeting Pt(IV) Derivatives of Cisplatin or Oxaliplatin Inhibit Tumor Growth in Mice without Inducing Neuropathic Pain	143
Targeting KAT6A/B as a New Therapeutic Strategy for Cancer Therapy	138
Targeting QPCTL: An Emerging Therapeutic Opportunity	138
Reaching Out and Moving Forward	132
Cell-Permeable Peptide Inhibitors of the p53-hDM2 Interaction via Foldamer Helix Mimicry and Bis-Thioether Stapling	128
Design and Synthesis of Novel Macrocyclic Derivatives as Potent and Selective Cyclin-Dependent Kinase 7 Inhibitors	128
Design, Synthesis, and Antitumor Activity Evaluation of 2-Phenylthiazole-5-Carboxylic Acid Derivatives Targeting Transactivation Response RNA-Binding Protein 2	120
Discovery of an Efficacious RET PROTAC Degrader with Enhanced Antiproliferative Activity against Resistant Cancer Cells Harboring RET Solvent-Front Mutations	119
Discovery of Novel 4,5,6,7-Tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one Derivatives as Orally Efficacious ATX Allosteric Inhibitors for the Treatment of Pulmonary Fibrosis	118
Structure-Based Discovery of a Highly Selective, Oral Polo-Like Kinase 1 Inhibitor with Potent Antileukemic Activity	114
Lactoferrin Nanoparticle-Vanadium Complex: A Promising High-Efficiency Agent against Glioblastoma by Triggering Autophagy and Ferroptosis	113
A Nurr1 Agonist Derived from the Natural Ligand DHI Induces Neuroprotective Gene Expression	110
Probing the Histamine H₁ Receptor Binding Site to Explore Ligand Binding Kinetics	109
Discovery of SILA-123 as a Highly Potent FLT3 Inhibitor for the Treatment of Acute Myeloid Leukemia with Various FLT3 Mutations	107
Probing the Biomolecular Interactions of DNA/HSA with the New Sn(IV) Complex and Computational Perspectives: Design, Synthesis, Characterization, Anticancer Activity, and Molecular Modeling Approach	105
Structure-Guided Discovery of Subtype Selective SIRT6 Inhibitors with a β-Carboline Skeleton for the Treatment of Breast Cancer	103

Discovery of Novel MyD88 Inhibitor A5S to Alleviate Acute Lung Injury with Favorable Drug-like Properties	102
Elaborate Structural Modifications Yielding Novel Boron-Containing N-Substituted Oseltamivir Derivatives as Potent Neuraminidase Inhibitors with Significantly Improved Broad-Spectrum Antiresistance Pr	102
Constrained β-Hairpins Targeting the EphA4 Ligand Binding Domain	101
Toward Dose Prediction at Point of Design	100
Celebrating John A. Katzenellenbogen, PhD and His Contributions to Science and Medicine	99
Fe(II)-Photoantibiotics for Potential Antibacterial, Antibiofilm, and Infective Wound Healing Applications in Rat Model	98
One-Pot Synthesis of Novel Tetrasubstituted α-Aminophosphonates Derived from α-Methylphosphoserine and In Vivo Evaluation as Anti-Inflammatory Agents	98
Imaging CDK4/6 Broaden Options of Breast Cancer Diagnostics with Positron Emission Tomography	97
Exploring Alternative Zinc-Binding Groups in Histone Deacetylase (HDAC) Inhibitors Uncovers DS-103 as a Potent Ethylhydrazide-Based HDAC Inhibitor with Chemosensitizing Properties	96
Artificial Intelligence in Natural Product Drug Discovery: Current Applications and Future Perspectives	96
An ²¹¹At-labeled Tetrazine for Pretargeted Therapy	96
Dissecting Structural Requirements of Leucinostatin A Derivatives for Antiprotozoal Activity and Mammalian Toxicity	95
BRF110, an Orally Active Nurr1-RXRα-Selective Rexinoid, Enhances BDNF Expression without Elevating Triglycerides	94
Discovery and Optimization of Pyrazine Carboxamide AZ3246, a Selective HPK1 Inhibitor	92
Procainamide–SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites	90
Synthetic Approaches to the New Drugs Approved During 2020	89
Network-Based Drug Optimization toward the Treatment of Parkinson’s Disease: NRF2, MAO-B, Oxidative Stress, and Chronic Neuroinflammation	88
Discovery of Potent Phosphodiesterase-9 Inhibitors for the Treatment of Hepatic Fibrosis	87
Structure-Based Design of a Chemical Probe Set for the 5-HT_5A Serotonin Receptor	87
Update on the Development of MNK Inhibitors as Therapeutic Agents	87
Targeting Glial Cells by Organic Anion-Transporting Polypeptide 1C1 (OATP1C1)-Utilizing l-Thyroxine-Derived Prodrugs	86
Rational Design of Original Fused-Cycle Selective Inhibitors of Tryptophan 2,3-Dioxygenase	86
Discovery of LYC-55716: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ) Agonist for Use in Treating Cancer	86
Comprehensive Insights into the Development of Antitoxoplasmosis Drugs: Current Advances, Obstacles, and Future Perspectives	84
Discovery of 3,5-Dimethyl-4-Sulfonyl-1H-Pyrrole-Based Myeloid Cell Leukemia 1 Inhibitors with High Affinity, Selectivity, and Oral Bioavailability	83
Development of First-in-Class Dual Sirt2/HDAC6 Inhibitors as Molecular Tools for Dual Inhibition of Tubulin Deacetylation	83
Design, Synthesis, and Biological Evaluation of Novel Hybrids Containing Dihydrochalcone as Tyrosinase Inhibitors to Treat Skin Hyperpigmentation	80
Discovery of MK-8153, a Potent and Selective ROMK Inhibitor and Novel Diuretic/Natriuretic	80
Antitumor Activity and Mechanistic Insights of a Mitochondria-Targeting Cu(I) Complex	80
Synthesis and Evaluation of a Monomethyl Auristatin E─Integrin α_vβ₆ Binding Peptide–Drug Conjugate for Tumor Targeted Drug Delivery	80
Design, Synthesis, Biological Evaluation, and Computational Studies of Novel Ureidopropanamides as Formyl Peptide Receptor 2 (FPR2) Agonists to Target the Resolution of Inflammation in Central Nervous	75
Discovery of Novel Dihydrothiopyrano[4,3-d]pyrimidine Derivatives as Potent HIV-1 NNRTIs with Significantly Reduced hERG Inhibitory Activity and Improved Resistance Profiles	75
Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors	74
Targeting Colorectal Cancer with Conjugates of a Glucose Transporter Inhibitor and 5-Fluorouracil	73
Site-Selective Antibody–Drug Conjugation by a Proximity-Driven S to N Acyl Transfer Reaction on a Therapeutic Antibody	72
Issue Publication Information	72
Issue Editorial Masthead	72
Issue Publication Information	70
Call for Papers: Exploring Covalent Modulators in Drug Discovery and Chemical Biology	70
Potent Zinc(II)-Based Immunogenic Cell Death Inducer Triggered by ROS-Mediated ERS and Mitochondrial Ca²⁺ Overload	69
Uncovering α-Selectivity for Liver X Receptor Agonists for Lipotoxic Cancer Therapies	68
PROTACs Targeting MLKL Protect Cells from Necroptosis	68
Discovery of Conformationally Constrained Dihydro Benzo-Indole Derivatives as Metallo-β-Lactamase Inhibitors to Tackle Multidrug-Resistant Bacterial Infections	67
Copper-KRAS-COX2 Axis: A Therapeutic Vulnerability in Pancreatic Cancer	67
Deconstruction of Dual-Site Tankyrase Inhibitors Provides Insights into Binding Energetics and Suggests Critical Hotspots for Ligand Optimization	67
Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions	67
Rezatapopt (PC14586): A First-in-Class Small Molecule p53 Y220C Mutant Protein Stabilizer in Clinical Trials	66
Discovery of CBPD-409 as a Highly Potent, Selective, and Orally Efficacious CBP/p300 PROTAC Degrader for the Treatment of Advanced Prostate Cancer	66
Issue Editorial Masthead	64
Correction to “Discovery of a Thiadiazole–Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models”	64

Issue Editorial Masthead	63
Issue Editorial Masthead	63
Issue Editorial Masthead	63
Targeted Degradation of HCV Polymerase by GalNAc-Conjugated ApTACs for Pan-Genotypic Antiviral Therapy with High Resistance Barriers	63
Issue Publication Information	63
Announcing the Latest Inductees to the ACS Division of Medicinal Chemistry Hall of Fame	62
Issue Publication Information	62
Correction to “A Novel, Selective c-Abl Inhibitor, Compound 5, Prevents Neurodegeneration in Parkinson’s Disease”	61
Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors	61
Correction to “Discovery and Structure-Based Optimization of Novel Atg4B Inhibitors for the Treatment of Castration-Resistant Prostate Cancer”	61
Identification of Diarylurea Inhibitors of the Cardiac-Specific Kinase TNNI3K by Designing Selectivity Against VEGFR2, p38α, and B-Raf	60
Small-Molecule Fluorescent Ligands for the CXCR4 Chemokine Receptor	59
Synthesis, In Vitro Profiling, and In Vivo Evaluation of Benzohomoadamantane-Based Ureas for Visceral Pain: A New Indication for Soluble Epoxide Hydrolase Inhibitors	59
Structure Activity Relationships for a Series of Eticlopride-Based Dopamine D₂/D₃ Receptor Bitopic Ligands	59
Novel Synthesis of C-Methylated Phytocannabinoids Bearing Anti-inflammatory Properties	59
New PSMA-Targeting Ligands: Transformation from Diagnosis (Ga-68) to Radionuclide Therapy (Lu-177)	59
Discovery of Novel Potent and Fast BTK PROTACs for the Treatment of Osteoclasts-Related Inflammatory Diseases	58
Unraveling the Promise of RET Inhibitors in Precision Cancer Therapy by Targeting RET Mutations	58
Comparison of the In Vitro and In Vivo Behavior of a Series of NIR-II-Emitting Aza-BODIPYs Containing Different Water-Solubilizing Groups and Their Trastuzumab Antibody Conjugates	58
Uncovering PROTAC Sensitivity and Efficacy by Multidimensional Proteome Profiling: A Case for STAT3	58
Discovery of Potent, Orally Bioavailable, Tricyclic NLRP3 Inhibitors	58
Hydrophobicity Determines the Bacterial Killing Rate of α-Helical Antimicrobial Peptides and Influences the Bacterial Resistance Development	57
Structure-Based Design and Characterization of the Highly Potent and Selective Covalent Inhibitors Targeting the Lysine Methyltransferases G9a/GLP	57
Synthesis, Optimization, and Structure–Activity Relationships of Imidazo[1,2-a]pyrimidines as Inhibitors of Group 2 Influenza A Viruses	57
SLL-627 Is a Highly Selective and Potent κ Opioid Receptor (KOR) Agonist with an Unexpected Nonreduction in Locomotor Activity	57
Potent, Selective, and Membrane Permeable 2-Amino-4-Substituted Pyridine-Based Neuronal Nitric Oxide Synthase Inhibitors	56
Membrane-Targeting Amphiphilic Honokiol Derivatives Containing an Oxazole Moiety as Potential Antibacterials against Methicillin-Resistant Staphylococcus aureus	56
Discovery of Triazolyl Derivatives of Cucurbitacin B Targeting IGF2BP1 against Non-Small Cell Lung Cancer	56
Discovery of a Novel Class of PROTACs as Potent and Selective Estrogen Receptor α Degraders to Overcome Endocrine-Resistant Breast Cancer In Vitro and In Vivo	56
Discovery of Potent and Selective Covalent Inhibitors of HER2^WT and HER2^YVMA	56
Pocket-to-Lead: Structure-Based De Novo Design of Novel Non-peptidic HIV-1 Protease Inhibitors Using the Ligand Binding Pocket as a Template	55
Discovery and Development of First-in-Class ACKR3/CXCR7 Superagonists for Platelet Degranulation Modulation	54
Development and Characterization of Potent Succinate Receptor Fluorescent Tracers	54
Selective HDAC3 Inhibitors with Potent In Vivo Antitumor Efficacy against Triple-Negative Breast Cancer	53
Discovery of BAY-390, a Selective CNS Penetrant Chemical Probe as Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonist	53
Biotin’s Lessons in Drug Design	53
Improvement of Oral Bioavailability of Pyrazolo-Pyridone Inhibitors of the Interaction of DCN1/2 and UBE2M	53
Discovery of the First-in-Class G9a/GLP PROTAC Degrader	53
Discovery, Optimization, and Preclinical Pharmacology of EP652, a METTL3 Inhibitor with Efficacy in Liquid and Solid Tumor Models	52
Discovery of Exceptionally Potent, Selective, and Efficacious PROTAC Degraders of CBP and p300 Proteins	52
Discovery of an Ortho-Substituted N-Cyclopropylmethyl-7α-phenyl-6,14-endoethano-tetrahydronorthebaine Derivative as a Selective and Potent Kappa Opioid Receptor Agonist with Subsided Sed	52
Secondary Structure Stabilization of Macrocyclic Antimicrobial Peptides via Cross-Link Swapping	52
Rational Design of a Novel Class of Human ClpP Agonists through a Ring-Opening Strategy with Enhanced Antileukemia Activity	52
Issue Editorial Masthead	51
Issue Publication Information	51
Issue Editorial Masthead	51
Oxetane Promise Delivered: Discovery of Long-Acting IDO1 Inhibitors Suitable for Q3W Oral or Parenteral Dosing	51
Issue Publication Information	51
Prodrug Strategies for the Development of β-l-5-((E)-2-Bromovinyl)-1-((2S,4S)-2-(hydroxymethyl)-1,3-(dioxolane-4-yl))uracil (l-BHDU) against Varicella Zoster	51
Issue Publication Information	51
Designing Small Molecule PI3Kγ Inhibitors: A Review of Structure-Based Methods and Computational Approaches	51
Discovery of LNP1892: A Precision Calcimimetic for the Treatment of Secondary Hyperparathyroidism	51
Issue Editorial Masthead	50
Issue Editorial Masthead	50
Issue Publication Information	50
Correction to “Discovery of First-in-Class Peptidomimetic Neurolysin Activators Possessing Enhanced Brain Penetration and Stability”	50
Issue Editorial Masthead	50
Issue Publication Information	49
Rethinking Medicinal Chemistry in the Cheminformatics Age	49
Discovery and Structure–Activity Relationships of Novel ssDAF-12 Receptor Modulators	49
Discovery and Characterization of a New Class of C5aR1 Antagonists Showing In Vivo Activity	49
Structure Guided Discovery of Novel Pan Metallo-β-Lactamase Inhibitors with Improved Gram-Negative Bacterial Cell Penetration	49
Issue Editorial Masthead	49
The New Frontier: Merging Molecular Glue Degrader and Antibody–Drug Conjugate Modalities To Overcome Strategic Challenges	48
Issue Publication Information	48
Discovery of a Series of 7-Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement	48
Assessing Darkness of the Human Kinome from a Medicinal Chemistry Perspective	48
Therapeutic Activity of the Lansoprazole Metabolite 5-Hydroxy Lansoprazole Sulfide in Triple-Negative Breast Cancer by Inhibiting the Enoyl Reductase of Fatty Acid Synthase	48
Discovery of a First-in-Class GPR183 Antagonist for the Potential Treatment of Rheumatoid Arthritis	48
Investigation of Janus Kinase (JAK) Inhibitors for Lung Delivery and the Importance of Aldehyde Oxidase Metabolism	48
Issue Publication Information	48
Identification of a Series of N-Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins	48
Development and Profiling of Inverse Agonist Tools for the Neuroprotective Transcription Factor Nurr1	48
Discovery of a Dual Tubulin and Neuropilin-1 (NRP1) Inhibitor with Potent In Vivo Anti-Tumor Activity via Pharmacophore-based Docking Screening, Structure Optimization, and Biological Evaluation	47
Designing Soluble PROTACs: Strategies and Preliminary Guidelines	47
Synthetic Biology Facilitates Semisynthetic Development of Type V Glycopeptide Antibiotics Targeting Vancomycin-Resistant Enterococcus	47
Targeting the Epidermal Growth Factor Receptor with Molecular Degraders: State-of-the-Art and Future Opportunities	47
High-Throughput Crystallography Reveals Boron-Containing Inhibitors of a Penicillin-Binding Protein with Di- and Tricovalent Binding Modes	47
Rational Design of RNA Demethylase FTO Inhibitors with Enhanced Antileukemia Drug-Like Properties	47
Development and In Vivo Evaluation of Small-Molecule Ligands for Positron Emission Tomography of Immune Checkpoint Modulation Targeting Programmed Cell Death 1 Ligand 1	47

Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y₁₄R Antagonist	47
Discovery of STAT3 and Histone Deacetylase (HDAC) Dual-Pathway Inhibitors for the Treatment of Solid Cancer	46
Polymeric Encapsulation of a Ru(II)-Based Photosensitizer for Folate-Targeted Photodynamic Therapy of Drug Resistant Cancers	46
In Memory of Professor Hualiang Jiang	45
Correction to “E3 Ligases Meet Their Match: Fragment-Based Approaches to Discover New E3 Ligands and to Unravel E3 Biology”	45
Cyanomethylquinolones as a New Class of Potential Multitargeting Broad-Spectrum Antibacterial Agents	45
Discovery of a Candidate Containing an (S)-3,3-Difluoro-1-(4-methylpiperazin-1-yl)-2,3-dihydro-1H-inden Scaffold as a Highly Potent Pan-Inhibitor of the BCR-ABL Kinase Including the T315	45
Development of MPS1 Inhibitors: Recent Advances and Perspectives	45
Probing Fluorinated Motifs onto Dual AChE-MAO B Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Early-ADME Studies	45
Design of Cell-Permeable Inhibitors of Eukaryotic Translation Initiation Factor 4E (eIF4E) for Inhibiting Aberrant Cap-Dependent Translation in Cancer	45
Issue Editorial Masthead	44
Photoredox-Mediated Immunotherapy Utilizing Rhenium(I) Photocatalysts with Electron Donor–Acceptor–Donor Configuration	44
DPP9 Comes of Age: Highly Selective Inhibitors Promise New Therapeutic Opportunities	44
Synthetic Approaches to the New Drugs Approved during 2023	44
Structure–Activity Relationship Studies of DNA Methyltransferase 1 Monovalent Degraders	43
Structure-Based Optimization of Pyridone α-Ketoamides as Inhibitors of the SARS-CoV-2 Main Protease	43
Rational Design, Synthesis, and Biological Evaluation of Novel c-Met Degraders for Lung Cancer Therapy	43
Discovery of N-(1,2,4-Thiadiazol-5-yl)benzo[b]oxepine-4-carboxamide Derivatives as Novel Antiresistance Androgen Receptor Antagonists	43
Tumor Microenvironment-Responsive Lipid Nanoparticle for Blocking Mitosis and Reducing Drug Resistance in NSCLC	43
Macrocyclization as a Strategy for Kinetic Solubility Improvement: A Comparative Analysis of Matched Molecular Pairs	43
Diagnostic and Therapeutic Radiopharmaceuticals: A “Hot” Topic	43
Recent Developments in 14–3–3 Stabilizers for Regulating Protein–Protein Interactions: An Update	43
Elucidation of Postfusion Structures of the Measles Virus F Protein for the Structure-Based Design of Fusion Inhibitors	43
Discovery of a Highly Selective BET BD2 Inhibitor from a DNA-Encoded Library Technology Screening Hit	43
Chemoproteomic Profiling of a Carbon-Stabilized Gold(III) Macrocycle Reveals Cellular Engagement with HMOX2	42
Engineered Cyclotide Blocks Neuronal Excitotoxicity	42
Redefining Antifungal Treatment: The Innovation of Metal-Based Compounds	42
Discovery of Novel Oxazolo[4,3-f]purine Derivatives as Antitumor Agents through PPIA Interaction	42
Mn-Specific Recognition of Guanidine Drives Selective Inhibition of Complex I	42
Correction to “Development of a Fluorescence Probe for High-Throughput Screening of Allosteric Inhibitors Targeting TRAP1”	42
Discovery of Nirmatrelvir (PF-07321332): A Potent, Orally Active Inhibitor of the Severe Acute Respiratory Syndrome Coronavirus 2 (SARS CoV-2) Main Protease	42
Discovery of Novel Pyrrolo[2,3-b]pyridine-Based CSF-1R Inhibitors with Demonstrated Efficacy against Patient-Derived Colorectal Cancer Organoids	42
Fragment-Based Drug Design: From Then until Now, and Toward the Future	42
Dual-Targeting TrxR-EGFR Alkynyl-Au(I) Gefitinib Complex Induces Ferroptosis in Gefitinib-Resistant Lung Cancer via Degradation of GPX4	42
Contilisant+Tubastatin A Hybrids: Polyfunctionalized Indole Derivatives as New HDAC Inhibitor-Based Multitarget Small Molecules with In Vitro and In Vivo Activity in Neurodegenerative Di	41
Discovery of TP0597850: A Selective, Chemically Stable, and Slow Tight-Binding Matrix Metalloproteinase-2 Inhibitor with a Phenylbenzamide–Pentapeptide Hybrid Scaffold	41
Issue Publication Information	41
Discovery of Ruthenium(II) Metallocompound and Olaparib Synergy for Cancer Combination Therapy	41
Design, Synthesis, and Anti-Cancer Evaluation of Novel Cyclic Phosphate Prodrug of Gemcitabine	41
Design, Synthesis, and Biological Activity of Novel Ornithine Decarboxylase (ODC) Inhibitors	41
Discovery of Darovasertib (NVP-LXS196), a Pan-PKC Inhibitor for the Treatment of Metastatic Uveal Melanoma	41
Discovery of β-Carboline Derivatives as a Highly Potent Cardioprotectant against Myocardial Ischemia-Reperfusion Injury	41
Oxygen-Dependent Interactions between the Ruthenium Cage and the Photoreleased Inhibitor in NAMPT-Targeted Photoactivated Chemotherapy	40
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes	40
Antioxidant, Anti-inflammatory, and Immunomodulatory Roles of Nonvitamin Antioxidants in Anti-SARS-CoV-2 Therapy	40
Ir(III) Half-Sandwich Photosensitizers with a π-Expansive Ligand for Efficient Anticancer Photodynamic Therapy	40
Spermine-Conjugated Short Proline-Rich Lipopeptides as Broad-Spectrum Intracellular Targeting Antibacterial Agents	40
Specific Inhibitors of Mitochondrial Deacylase Sirtuin 4 Endowed with Cellular Activity	40
Discovery and Structure-Based Design of Inhibitors of the WD Repeat-Containing Protein 5 (WDR5)–MYC Interaction	40
First GPR119 PET Imaging Ligand: Synthesis, Radiochemistry, and Preliminary Evaluations	39
Thermal Proteome Profiling Strategy Identifies CNPY3 as a Cellular Target of Gambogic Acid for Inducing Prostate Cancer Pyroptosis	39
Discovery of Benzo[d]oxazoles as Novel Dual Small-Molecule Inhibitors Targeting PD-1/PD-L1 and VISTA Pathway	39
Discovery of a Novel CRBN-Recruiting cGAS PROTAC Degrader for the Treatment of Ulcerative Colitis	39
Does the Number of Bifunctional Chelators Conjugated to a mAb Affect the Biological Activity of Its Radio-Labeled Counterpart? Discussion Using the Example of mAb against CD-20 Labeled with ⁹⁰	39
Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases	39
Alicyclic Ring Size Variation of 4-Phenyl-2-naphthoic Acid Derivatives as P2Y₁₄ Receptor Antagonists	39
The Discovery of Exarafenib (KIN-2787): Overcoming the Challenges of Pan-RAF Kinase Inhibition	39
New Insights into the Structure–Activity Relationship and Neuroprotective Profile of Benzodiazepinone Derivatives of Neurounina-1 as Modulators of the Na⁺/Ca²⁺ Exchanger I	39
Discovery and Evaluation of TLR-Targeted Immune Agonists	39
Development of CD73 Inhibitors in Tumor Immunotherapy and Opportunities in Imaging and Combination Therapy	39
Discovery of Apararenone (MT-3995) as a Highly Selective, Potent, and Novel Nonsteroidal Mineralocorticoid Receptor Antagonist	39
CBP/p300 Degrader: A Promising Therapeutic Strategy for Treatment of Prostate Cancer and Beyond	38
First Demonstration of In Vivo PDE11A4 Target Engagement for Potential Treatment of Age-Related Memory Disorders	38
Chiral Alkyl Groups at Position 3(1′) of Pyropheophorbide-a Specify Uptake and Retention by Tumor Cells and Are Essential for Effective Photodynamic Therapy	38
Structure-Based Design and Development of Phosphine Oxides as a Novel Chemotype for Antibiotics that Dysregulate Bacterial ClpP Proteases	38
Discovery and Preclinical Characterization of Usmarapride (SUVN-D4010): A Potent, Selective 5-HT₄ Receptor Partial Agonist for the Treatment of Cognitive Deficits Associated with Alzheimer’	38
Therapeutic Potential of a Water-Soluble Silver-Diclofenac Coordination Polymer on 3D Pancreatic Cancer Spheroids	38
Why All the Fury over Furin?	38
Correction to “Discovery of a Series of Hydroxamic Acid-Based Microtubule Destabilizing Agents with Potent Antitumor Activity”	38
Discovery of Novel UDP-N-Acetylglucosamine Acyltransferase (LpxA) Inhibitors with Activity against Pseudomonas aeruginosa	38
Iterative Optimization and Structure–Activity Relationship Studies of Oseltamivir Amino Derivatives as Potent and Selective Neuraminidase Inhibitors via Targeting 150-Cavity	38
Novel Aryl-Substituted Pyrimidones as Inhibitors of 3-Mercaptopyruvate Sulfurtransferase with Antiproliferative Efficacy in Colon Cancer	38
Structure–Activity Relationship Studies in Benzothiadiazoles as Novel Vaccine Adjuvants	38
Design, Synthesis, and Biological Evaluation of a Novel Photocaged PI3K Inhibitor toward Precise Cancer Treatment	37
Discovery of 5-Phenylpyrazolopyrimidinone Analogs as Potent Antitrypanosomal Agents with In Vivo Efficacy	37
Synthetic Anti-Cocaine Nanoaccine Successfully Prevents Cocaine-Induced Hyperlocomotion	37
4′-Ethynyl-2′-deoxy-2′-β-fluoro-2-fluoroadenosine: A Highly Potent and Orally Available Clinical Candidate for the Treatment of HIV-1 Infection	37
Rationally Designed Amanitins Achieve Enhanced Cytotoxicity	37
Design, Synthesis, and Biological Activity of New CB2 Receptor Ligands: from Orthosteric and Allosteric Modulators to Dualsteric/Bitopic Ligands	37
Discovery of Hyperstable Noncanonical Plant-Derived Epidermal Growth Factor Receptor Agonist and Analogs	37
The Design, Synthesis, and Evaluation of Novel 9-Arylxanthenedione-Based Allosteric Modulators for the δ-Opioid Receptor	37
Design, Synthesis, and Biological Evaluation of Covalently Mucoadhesive Derivatives as Nonsystemic Intestine-Targeted TGR5 Agonists	37
d-Peptidase Activity in a Marine Mollusk Detoxifies a Nonribosomal Cyclic Lipopeptide: An Ecological Model to Study Antibiotic Resistance	37
Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance	37
Neuroactive Type-A γ-Aminobutyric Acid Receptor Allosteric Modulator Steroids from the Hypobranchial Gland of Marine Mollusk, Conus geographus	37
Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2)	37
Rational Design of Sulfonyl-γ-AApeptides as Highly Potent HIV-1 Fusion Inhibitors with Broad-Spectrum Activity	36
Discovery, SAR Study of GST Inhibitors from a Novel Quinazolin-4(1H)-one Focused DNA-Encoded Library	36
Developing an Arene Binuclear Ruthenium(II) Complex to Induce Ferroptosis and Activate the cGAS-STING Pathway: Targeted Inhibiting Growth and Metastasis of Triple Negative Breast Cancer	36
Selective and Orally Bioavailable c-Met PROTACs for the Treatment of c-Met-Addicted Cancer	36
mARC1 Is the Main Contributor to Metabolic Reduction of N-Hydroxyurea	36
Exploring Heteroaromatic Rings as a Replacement for the Labile Amide of Antiplasmodial Pantothenamides	36
Synthesis and Conformational Analysis of FR901464-Based RNA Splicing Modulators and Their Synergism in Drug-Resistant Cancers	36
Discovery of Novel 7-Azaindole Derivatives as Selective Covalent Fibroblast Growth Factor Receptor 4 Inhibitors for the Treatment of Hepatocellular Carcinoma	36
A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia	36