OOIR: Observatory of International Research

Papers

(The H4-Index of Journal of Medicinal Chemistry is 67. 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 2021-09-01 to 2025-09-01.)

Article	Citations
Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate	521
Dissecting Structural Requirements of Leucinostatin A Derivatives for Antiprotozoal Activity and Mammalian Toxicity	457
Sertraline and Astemizole Enhance the Deubiquitinase Activity of USP7 by Binding to Its Switching Loop Region	451
Elaborate Structural Modifications Yielding Novel Boron-Containing N-Substituted Oseltamivir Derivatives as Potent Neuraminidase Inhibitors with Significantly Improved Broad-Spectrum Antiresistance Pr	336
NSAID–Au(I) Complexes Induce ROS-Driven DAMPs and Interpose Inflammation to Stimulate the Immune Response against Ovarian Cancer	283
Discovery, SAR Study of GST Inhibitors from a Novel Quinazolin-4(1H)-one Focused DNA-Encoded Library	220
A First-in-Class Pyrazole-isoxazole Enhanced Antifungal Activity of Voriconazole: Synergy Studies in an Azole-Resistant Candida albicans Strain, Computational Investigation and in Vivo Validati	195
Efficacy, Mechanism, and Structure–Activity Relationship of 6-Methoxy Benzofuran Derivatives as a Useful Tool for Senile Osteoporosis	176
Design, Synthesis, and Biological Activity of Novel Ornithine Decarboxylase (ODC) Inhibitors	166
Mn-Specific Recognition of Guanidine Drives Selective Inhibition of Complex I	156
Structure-Based Design of Novel Alkynyl Thio-Benzoxazepinone Receptor-Interacting Protein Kinase-1 Inhibitors: Extending the Chemical Space from the Allosteric to ATP Binding Pockets	154
Discovery of 5-Phenylpyrazolopyrimidinone Analogs as Potent Antitrypanosomal Agents with In Vivo Efficacy	150
Diamino Allose Phosphates: Novel, Potent, and Highly Stable Toll-like Receptor 4 Agonists	150
Further Studies on the Highly Active Des-C-Ring and Aromatic-D-Ring Analogues of 1α,25-Dihydroxyvitamin D₃ (Calcitriol): Refinement of the Side Chain	142
Discovery of Novel 2-Oxoacetamide Derivatives as B3GAT3 Inhibitors for the Treatment of Hepatocellular Carcinoma	139
Structure-Based Design and Synthesis of Covalent Inhibitors for Deubiquitinase and Acetyltransferase ChlaDUB1 of Chlamydia trachomatis	135
A Photoactivatable Version of Ivabradine Enables Light-Induced Block of HCN Current In Vivo	135
Novel Medicinal Chemistry Strategies Targeting CDK5 for Drug Discovery	128
Multidisciplinary Training for Fostering Next-Generation Medicinal Chemists	124
CRCM5484: A BET-BDII Selective Compound with Differential Anti-leukemic Drug Modulation	122
Dual A1/A3 Adenosine Receptor Antagonists: Binding Kinetics and Structure−Activity Relationship Studies Using Mutagenesis and Alchemical Binding Free Energy Calculations	122
Cell-Based Screen Identifies a Highly Potent and Orally Available ABCB1 Modulator for Treatment of Multidrug Resistance	119
Mechanistic Investigation of Thiazole-Based Pyruvate Kinase M2 Inhibitor Causing Tumor Regression in Triple-Negative Breast Cancer	116
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	113
Rezatapopt (PC14586): A First-in-Class Small Molecule p53 Y220C Mutant Protein Stabilizer in Clinical Trials	112

Heparan Sulfate-Based Neoproteoglycan for Targeted Lysosomal Degradation of Amyloid-β	109
Iterative Optimization and Structure–Activity Relationship Studies of Oseltamivir Amino Derivatives as Potent and Selective Neuraminidase Inhibitors via Targeting 150-Cavity	105
All-d-Enantiomeric Peptide D3 Designed for Alzheimer’s Disease Treatment Dynamically Interacts with Membrane-Bound Amyloid-β Precursors	104
Selective and Orally Bioavailable c-Met PROTACs for the Treatment of c-Met-Addicted Cancer	103
Structure–Activity Relationships of Truncated 1′-Homologated Carbaadenosine Derivatives as New PPARγ/δ Ligands: A Study on Sugar Puckering Affecting Binding to PPARs	101
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	100
Antibody-Vincristine Conjugates as Potent Anticancer Therapeutic Agents	100
Navigating the Landscape of Academic Drug Discovery: An 18-Year Journey	100
Rapid Response Antimicrobial Peptide Design Strategy Driven by Meta-Learning for Emerging Drug-Resistant Pathogens	95
Chemical Toolkit for PARK7: Potent, Selective, and High-Throughput	95
Discovery of Ruthenium(II) Metallocompound and Olaparib Synergy for Cancer Combination Therapy	94
Macrocyclization as a Strategy for Kinetic Solubility Improvement: A Comparative Analysis of Matched Molecular Pairs	93
Discovery of the Clinical Candidate S-892216: A Second-Generation of SARS-CoV-2 3CL Protease Inhibitor for Treating COVID-19	91
Discovery of Covalent MLKL PROTAC Degraders via Optimization of a Theophylline Derivative Ligand for Treating Necroptosis	91
The Design, Synthesis, and Evaluation of Novel 9-Arylxanthenedione-Based Allosteric Modulators for the δ-Opioid Receptor	91
Diagnostic and Therapeutic Radiopharmaceuticals: A “Hot” Topic	87
Correction to “Discovery of a Thiadiazole–Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models”	86
Discovery and Optimization of Selective Brain-Penetrant EBP Inhibitors that Enhance Oligodendrocyte Formation	85
Exploring Structural Determinants of Bias among D4 Subtype-Selective Dopamine Receptor Agonists	85
In Silico Assisted Identification, Synthesis, and In Vitro Pharmacological Characterization of Potent and Selective Blockers of the Epilepsy-Associated KCNT1 Channel	83
Rational Design, Synthesis, and Biological Evaluation of Novel S1PR2 Antagonists for Reversing 5-FU-Resistance in Colorectal Cancer	83
Discovery of 3-(Fluoro-imidazolyl)pyridazine Derivatives as Potent STING Agonists with Antitumor Activity	83
Synthesis and Evaluation of a Monomethyl Auristatin E─Integrin α_vβ₆ Binding Peptide–Drug Conjugate for Tumor Targeted Drug Delivery	82
Structure-Based Optimization of Pyridone α-Ketoamides as Inhibitors of the SARS-CoV-2 Main Protease	82
Aldo-Keto Reductase 1C3 Inhibitor Prodrug Improves Pharmacokinetic Profile and Demonstrates In Vivo Efficacy in a Prostate Cancer Xenograft Model	80
Discovery of Highly Selective CYP1B1 Inhibitors	79
Design and Synthesis of PARP/CDK6 Dual-Target Inhibitors Modulating of Wnt/β-Catenin Signaling Pathway for the Treatment of BRCA Wild-Type TNBC	79
Improvement of the Metabolic Stability of GPR88 Agonist RTI-13951-33: Design, Synthesis, and Biological Evaluation	78
Discovery of Selective Histone Deacetylase 1 and 2 Inhibitors: Screening of a Focused Library Constructed by Click Chemistry, Kinetic Binding Analysis, and Biological Evaluation	76
New Pqs Quorum Sensing System Inhibitor as an Antibacterial Synergist against Multidrug-Resistant Pseudomonas aeruginosa	76
Discovery and Mechanism of SARS-CoV-2 Main Protease Inhibitors	75
Issue Publication Information	74
Issue Editorial Masthead	74
Discovery of RP-1664: A First-in-Class Orally Bioavailable, Selective PLK4 Inhibitor	73
Issue Editorial Masthead	73
Development of CD73 Inhibitors in Tumor Immunotherapy and Opportunities in Imaging and Combination Therapy	72
Micromonospora: A Prolific Source of Bioactive Secondary Metabolites with Therapeutic Potential	71
Macrocyclic Neutralizer to Polybrene via Direct Host–Guest Complexation	70
Discovery of Exceptionally Potent, Selective, and Efficacious PROTAC Degraders of CBP and p300 Proteins	69
Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib	68
N-Terminus to Arginine Side-Chain Cyclization of Linear Peptidic Neuropeptide Y Y₄ Receptor Ligands Results in Picomolar Binding Constants	67
Structure-Based Drug Design of ADRA2A Antagonists Derived from Yohimbine	67
Carboxylesterase-Triggered Theranostic Agent: Advancing Near-Infrared Imaging and Therapeutic Efficacy in Hepatocellular Carcinoma	67
Design, Synthesis, and Pharmacological Evaluation of Biaryl-Containing PD-1/PD-L1 Interaction Inhibitors Bearing a Unique Difluoromethyleneoxy Linkage	67