OOIR: Observatory of International Research

Papers

(The H4-Index of Journal of Medicinal Chemistry is 69. 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 2022-06-01 to 2026-06-01.)

Article	Citations
pH-Responsive Self-Assembled Upconversion Photosensitizer and RSL3 Synergistically Induce Tumor Ferroptosis	766
Unmasking Conformationally Adaptable Lipids as Drug Receptors	402
Mn-Specific Recognition of Guanidine Drives Selective Inhibition of Complex I	268
Issue Editorial Masthead	231
Aldo-Keto Reductase 1C3 Inhibitor Prodrug Improves Pharmacokinetic Profile and Demonstrates In Vivo Efficacy in a Prostate Cancer Xenograft Model	198
Turning the Spotlight Away from PDT: Chemodynamic Dominance of 2-(2-Bromopyridin-4-yl)-1 H -imidazo[4,5- f	192
Discovery of Cdc20/Hsp90 Dual-Target Inhibitors with Potent Antitumor Activity for Therapy of Acquired Resistant Melanoma	164
Optimization of 2,8-Diaryl-1,5-naphthyridines as Plasmodium falciparum Phosphatidylinositol 4-Kinase Inhibitors with Improved ADME Profiles and In Vivo E	163
Discovery of 5-Phenylpyrazolopyrimidinone Analogs as Potent Antitrypanosomal Agents with In Vivo Efficacy	163
Structure-Based Design and Synthesis of Covalent Inhibitors for Deubiquitinase and Acetyltransferase ChlaDUB1 of Chlamydia trachomatis	162
Multidisciplinary Training for Fostering Next-Generation Medicinal Chemists	149
A Photoactivatable Version of Ivabradine Enables Light-Induced Block of HCN Current In Vivo	144
Small-Molecule Fluorescent Ligands for the CXCR4 Chemokine Receptor	140
Probing Guanidino Pendant or Bridged Groups in Cyclic Antimicrobial Peptides Derived from Temporin L: A Strategy to Improve Efficacy against Gram-Negative Bacteria	131
Correction to “Discovery of a Thiadiazole–Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models”	126
Discovery of the First-In-Class HSD17B13/PPAR Multitarget Modulators for the Treatment of Metabolic Dysfunction-Associated Steatohepatitis	124
Navigating the Landscape of Academic Drug Discovery: An 18-Year Journey	124
Toward Dose Prediction at Point of Design	122
Therapeutic Potential of Novel Antimicrobial Peptide Pap12-6-10: Mechanisms of Antibacterial and Anti-inflammatory Action Against Gram-Negative Sepsis	119
Targeting Toll-like Receptors 7, 8, and 9 Inhibition in Systemic Lupus Erythematosus: Therapeutic Advance and Future Directions	119
Accurate Prediction of Core-Hopping Transformations Using Molecular Dynamics-Derived Conformational Ensembles: Application to the Discovery of Novel P2X3 Antagonists	112
AKR1C3 Inhibition: A Strategy to Reverse Osimertinib Resistance in Non-small Cell Lung Cancer	109
Antiviral Protein–Protein Interaction Inhibitors	104
GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A_2A Adenosine Receptor	102
Discovery of YFJ-36: Design, Synthesis, and Antibacterial Activities of Catechol-Conjugated β-Lactams against Gram-Negative Bacteria	102

Synthesis and Structure–Activity Relationships of 2,5-Dimethoxy-4-Substituted Phenethylamines and the Discovery of CYB210010: A Potent, Orally Bioavailable and Long-Acting Serotonin 5-HT₂ R	102
Discovery, SAR Study of GST Inhibitors from a Novel Quinazolin-4(1H)-one Focused DNA-Encoded Library	100
Structure–Activity Relationship Guided Scaffold Hopping Resulted in the Identification of GLPG4970, a Highly Potent Dual SIK2/SIK3 Inhibitor	93
Antibody-Vincristine Conjugates as Potent Anticancer Therapeutic Agents	93
Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2)	90
Fragment-Based Development of Small Molecule Inhibitors Targeting Mycobacterium tuberculosis Cholesterol Metabolism	90
Progress on the Pharmacological Targeting of Janus Pseudokinases	89
Discovery of Exceptionally Potent, Selective, and Efficacious PROTAC Degraders of CBP and p300 Proteins	89
Discovery of Furan-2-Carboxylic Acid Derivatives as Novel D-Dopachrome Tautomerase (D-DT) and Macrophage Migration Inhibitory Factor-1 (MIF-1) Dual Inhibitors	88
Subtle Structural Changes across the Boundary between A_2AR/A_2BR Dual Antagonism and A_2BR Antagonism: A Novel Class of 2-Aminopyrimidine-Based Derivatives	88
Diagnostic and Therapeutic Radiopharmaceuticals: A “Hot” Topic	88
Sertraline and Astemizole Enhance the Deubiquitinase Activity of USP7 by Binding to Its Switching Loop Region	88
Bioactivity-Driven Synthesis of the Marine Natural Product Naamidine J and Its Derivatives as Potential Tumor Immunological Agents by Inhibiting Programmed Death-Ligand 1	86
Drug Repurposing: Conversion of the Peripherally Restricted HIV Protease Inhibitor Amprenavir to Potent, Selective, and CNS-Penetrant Agonists for the Cannabinoid Receptor 2	85
Carboxylesterase-Triggered Theranostic Agent: Advancing Near-Infrared Imaging and Therapeutic Efficacy in Hepatocellular Carcinoma	83
Elaborate Structural Modifications Yielding Novel Boron-Containing N-Substituted Oseltamivir Derivatives as Potent Neuraminidase Inhibitors with Significantly Improved Broad-Spectrum Antiresistance Pr	82
Discovery of 2-(Pyrazol-4-yl)-quinazolin-4(3H)-one Derivatives as Subnanomolar BRD4 BD2 Inhibitors with High Selectivity via a Bioisosterism Approach	81
Selective and Orally Bioavailable c-Met PROTACs for the Treatment of c-Met-Addicted Cancer	81
Novel Medicinal Chemistry Strategies Targeting CDK5 for Drug Discovery	80
Discovery of a Highly Potent and Selective Small-Molecule Inhibitor of In Vivo Anaerobic Choline Metabolism by Human Gut Bacteria	80
Discovery and Optimization of Selective Brain-Penetrant EBP Inhibitors that Enhance Oligodendrocyte Formation	77
Discovery of Novel 2-Oxoacetamide Derivatives as B3GAT3 Inhibitors for the Treatment of Hepatocellular Carcinoma	77
Design and Synthesis of PARP/CDK6 Dual-Target Inhibitors Modulating of Wnt/β-Catenin Signaling Pathway for the Treatment of BRCA Wild-Type TNBC	77
Steric Blockade of Oxy-Myoglobin Oxidation by Thiosemicarbazones: Structure–Activity Relationships of the Novel PPP4pT Series	76
N-Heterocyclic 3-Pyridyl Carboxamide Inhibitors of DHODH for the Treatment of Acute Myelogenous Leukemia	76
How a Medicinal Chemistry Project Changed the Way Prostate Cancer is Diagnosed and Treated	75
Dissecting Structural Requirements of Leucinostatin A Derivatives for Antiprotozoal Activity and Mammalian Toxicity	74
Design, Synthesis, and Biological Evaluation of an Orally Bioavailable, Potent, and Selective ROCK2 Inhibitor for Psoriasis Treatment	74
The New Frontier: Merging Molecular Glue Degrader and Antibody–Drug Conjugate Modalities To Overcome Strategic Challenges	73
Exploring Structural Determinants of Bias among D4 Subtype-Selective Dopamine Receptor Agonists	73
Diamino Allose Phosphates: Novel, Potent, and Highly Stable Toll-like Receptor 4 Agonists	71
Dual A1/A3 Adenosine Receptor Antagonists: Binding Kinetics and Structure−Activity Relationship Studies Using Mutagenesis and Alchemical Binding Free Energy Calculations	71
Rezatapopt (PC14586): A First-in-Class Small Molecule p53 Y220C Mutant Protein Stabilizer in Clinical Trials	71
Chemical Toolkit for PARK7: Potent, Selective, and High-Throughput	71
Micromonospora: A Prolific Source of Bioactive Secondary Metabolites with Therapeutic Potential	70
Small Molecule Inhibitors Targeting the “Undruggable” Survivin: The Past, Present, and Future from a Medicinal Chemist’s Perspective	70
Discovery of RP-1664: A First-in-Class Orally Bioavailable, Selective PLK4 Inhibitor	70
The Design, Synthesis, and Evaluation of Novel 9-Arylxanthenedione-Based Allosteric Modulators for the δ-Opioid Receptor	70
Akt Inhibitor Advancements: From Capivasertib Approval to Covalent-Allosteric Promises	69
Identification of Non-competitive and Reversible Inhibitors of Glycine Transporter 2: A Promising Non-opioid Therapeutic Strategy for Neuropathic Pain	69
Rapid Response Antimicrobial Peptide Design Strategy Driven by Meta-Learning for Emerging Drug-Resistant Pathogens	69
Optimization of Chelator Conjugation to PD-1/VEGF Bispecific Antibody for ⁸⁹ Zr-ImmunoPET Imaging	69
Rational Design of Schiff Base Copper Chelators as Potent Necroptosis Inducers for Anticancer Therapy	69
Spacial Score─A Comprehensive Topological Indicator for Small-Molecule Complexity	69