ACS Medicinal Chemistry Letters

Article	Citations
Identification of 14 Known Drugs as Inhibitors of the Main Protease of SARS-CoV-2	165
Advantages of the Parent Nucleoside GS-441524 over Remdesivir for Covid-19 Treatment	137
Solution Conformations Shed Light on PROTAC Cell Permeability	95
Understanding and Improving the Membrane Permeability of VH032-Based PROTACs	77
The Advent of Generative Chemistry	64
Visible-Light Photocatalysis as an Enabling Technology for Drug Discovery: A Paradigm Shift for Chemical Reactivity	64
Structural Impact of Mutation D614G in SARS-CoV-2 Spike Protein: Enhanced Infectivity and Therapeutic Opportunity	61
PROTAC Compounds Targeting α-Synuclein Protein for Treating Neurogenerative Disorders: Alzheimer’s and Parkinson’s Diseases	53
A Role for Metal-Based Drugs in Fighting COVID-19 Infection? The Case of Auranofin	52
Steering New Drug Discovery Campaigns: Permeability, Solubility, and Physicochemical Properties in the bRo5 Chemical Space	51
Ultra-High-Throughput Acoustic Droplet Ejection-Open Port Interface-Mass Spectrometry for Parallel Medicinal Chemistry	47
Therapeutic Potential of Targeted Nanoparticles and Perspective on Nanotherapies	46
Discovery of Potent and Orally Available Bicyclo[1.1.1]pentane-Derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors	45
Biotransformation: Impact and Application of Metabolism in Drug Discovery	44
Direct-to-Biology Accelerates PROTAC Synthesis and the Evaluation of Linker Effects on Permeability and Degradation	44
Discovery of CPI-1612: A Potent, Selective, and Orally Bioavailable EP300/CBP Histone Acetyltransferase Inhibitor	43
Decarboxylative Cross-Coupling: A Radical Tool in Medicinal Chemistry	41
Risdiplam, the First Approved Small Molecule Splicing Modifier Drug as a Blueprint for Future Transformative Medicines	41
Systematic Investigation of the Permeability of Androgen Receptor PROTACs	40
Evaluation of 3-Dimensionality in Approved and Experimental Drug Space	39
Optimization of Triarylpyridinone Inhibitors of the Main Protease of SARS-CoV-2 to Low-Nanomolar Antiviral Potency	37
The Growing Importance of Chirality in 3D Chemical Space Exploration and Modern Drug Discovery Approaches for Hit-ID	36
Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate	36
Design and Evaluation of Bispidine-Based SARS-CoV-2 Main Protease Inhibitors	35
Design, Synthesis, and Biological Evaluation of Imidazopyridines as PD-1/PD-L1 Antagonists	31

Folate Receptor Targeting and Cathepsin B-Sensitive Drug Delivery System for Selective Cancer Cell Death and Imaging	31
Allosteric Modulation of Protein Arginine Methyltransferase 5 (PRMT5)	30
Simultaneous Inhibition of SIRT2 Deacetylase and Defatty-Acylase Activities via a PROTAC Strategy	29
Ulotaront: A TAAR1 Agonist for the Treatment of Schizophrenia	28
Structural Insights into Plasticity and Discovery of Remdesivir Metabolite GS-441524 Binding in SARS-CoV-2 Macrodomain	28
Discovery of CA-4948, an Orally Bioavailable IRAK4 Inhibitor for Treatment of Hematologic Malignancies	27
Influence of Linker Attachment Points on the Stability and Neosubstrate Degradation of Cereblon Ligands	27
Complex Crystal Structures of EGFR with Third-Generation Kinase Inhibitors and Simultaneously Bound Allosteric Ligands	27
Discovery of Highly Selective and Potent HDAC3 Inhibitors Based on a 2-Substituted Benzamide Zinc Binding Group	26
Asymmetrically Substituted Quadruplex-Binding Naphthalene Diimide Showing Potent Activity in Pancreatic Cancer Models	26
Blocking Coronavirus 19 Infection via the SARS-CoV-2 Spike Protein: Initial Steps	26
Discovery of Dotinurad (FYU-981), a New Phenol Derivative with Highly Potent Uric Acid Lowering Activity	25
Emerging Chromatography-Free High-Throughput Mass Spectrometry Technologies for Generating Hits and Leads	25
Characterization of Specific N-α-Acetyltransferase 50 (Naa50) Inhibitors Identified Using a DNA Encoded Library	25
Chiral Analogues of PFI-1 as BET Inhibitors and Their Functional Role in Myeloid Malignancies	25
Rational Control of Molecular Properties Is Mandatory to Exploit the Potential of PROTACs as Oral Drugs	25
Trends in Hit-to-Lead Optimization Following DNA-Encoded Library Screens	24
Selective Covalent Targeting of Mutated EGFR(T790M) with Chlorofluoroacetamide-Pyrimidines	24
Benzoxaboroles: New Potent Inhibitors of the Carbonic Anhydrases of the Pathogenic Bacterium Vibrio cholerae	24
SD-91 as A Potent and Selective STAT3 Degrader Capable of Achieving Complete and Long-Lasting Tumor Regression	24
Discovery of Potent and Orally Bioavailable Small Molecule Antagonists of Toll-like Receptors 7/8/9 (TLR7/8/9)	24
Establishing the Structure–Activity Relationship of Daptomycin	24
Spiroindoline-Capped Selective HDAC6 Inhibitors: Design, Synthesis, Structural Analysis, and Biological Evaluation	23
Trisubstituted Pyrrolinones as Small-Molecule Inhibitors Disrupting the Protein–RNA Interaction of LIN28 and Let-7	23
On the Selectivity of Heparan Sulfate Recognition by SARS-CoV-2 Spike Glycoprotein	23
Evaluation of 5-(Trifluoromethyl)-1,2,4-oxadiazole-Based Class IIa HDAC Inhibitors for Huntington’s Disease	23
GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family	23
A Warhead Substitution Study on the Coronavirus Main Protease Inhibitor Nirmatrelvir	23
Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting Del19/T790M/C797S Mutation	23
Design, Synthesis, and Biological Evaluation of IRAK4-Targeting PROTACs	22
Rationally Designed Covalent BCL6 Inhibitor That Targets a Tyrosine Residue in the Homodimer Interface	22
2-Cyanoisonicotinamide Conjugation: A Facile Approach to Generate Potent Peptide Inhibitors of the Zika Virus Protease	21
P2Y14 Receptor Antagonists Reverse Chronic Neuropathic Pain in a Mouse Model	21
Peripherally Crowded Cationic Phthalocyanines as Efficient Photosensitizers for Photodynamic Therapy	21
Intriguing Antiviral Modified Nucleosides: A Retrospective View into the Future Treatment of COVID-19	21
De-risking Drug Discovery of Intracellular Targeting Peptides: Screening Strategies to Eliminate False-Positive Hits	21
Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance	20
Discovery of the First Orally Available, Selective KNa1.1 Inhibitor: In Vitro and In Vivo Activity of an Oxadiazole Series	20
Beyond 20 in the 21st Century: Prospects and Challenges of Non-canonical Amino Acids in Peptide Drug Discovery	20
Exploring the Chemical Space of Benzothiazole-Based DNA Gyrase B Inhibitors	20
GPCR Inhibition in Treating Lymphoma	19
Chemical Modification of Linkers Provides Stable Linker–Payloads for the Generation of Antibody–Drug Conjugates	19
Development of a Hematopoietic Prostaglandin D Synthase-Degradation Inducer	19
Discovery of Investigational Drug CT1812, an Antagonist of the Sigma-2 Receptor Complex for Alzheimer’s Disease	19
Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer	19
Discovery of Orally Active Isofuranones as Potent, Selective Inhibitors of Hematopoetic Progenitor Kinase 1	19
2-Aminooxazole as a Novel Privileged Scaffold in Antitubercular Medicinal Chemistry	18
Discovery of Diaminopyrimidine Carboxamide HPK1 Inhibitors as Preclinical Immunotherapy Tool Compounds	18
Exploring the Implication of DDX3X in DENV Infection: Discovery of the First-in-Class DDX3X Fluorescent Inhibitor	18
Structural Approach to Assessing the Innovativeness of New Drugs Finds Accelerating Rate of Innovation	18

Characterization of an Alginate Encapsulated LS180 Spheroid Model for Anti-colorectal Cancer Compound Screening	18
ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model	18
Artemisinin Derivatives with Antimelanoma Activity Show Inhibitory Effect against Human DNA Topoisomerase 1	18
Discovery of TAK-925 as a Potent, Selective, and Brain-Penetrant Orexin 2 Receptor Agonist	18
Remodelin Is a Cryptic Assay Interference Chemotype That Does Not Inhibit NAT10-Dependent Cytidine Acetylation	17
Design and Implementation of Synthetic RNA Binders for the Inhibition of miR-21 Biogenesis	17
Combined Peptide and Small-Molecule Approach toward Nonacidic THIQ Inhibitors of the KEAP1/NRF2 Interaction	17
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2	17
Antiferroptotic Activity of Phenothiazine Analogues: A Novel Therapeutic Strategy for Oxidative Stress Related Disease	17
BMS-813160: A Potent CCR2 and CCR5 Dual Antagonist Selected as a Clinical Candidate	17
Cell Permeability of Isomeric Macrocycles: Predictions and NMR Studies	17
Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors	17
Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors	17
Novel Betulinic Acid–Nucleoside Hybrids with Potent Anti-HIV Activity	17
Design, Synthesis, and Biological Evaluation of Novel Acylhydrazone Derivatives as Potent Neuraminidase Inhibitors	17
Contemporary Computational Applications and Tools in Drug Discovery	17
Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1)	17
Development of Chimeric Molecules That Degrade the Estrogen Receptor Using Decoy Oligonucleotide Ligands	16
Resorufin Enters the Photodynamic Therapy Arena: A Monoamine Oxidase Activatable Agent for Selective Cytotoxicity	16
Influence of 4′-Substitution on the Activity of Gemcitabine and Its ProTide Against VZV and SARS-CoV-2	16
Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1	16
Pilot Study to Quantify Palladium Impurities in Lead-like Compounds Following Commonly Used Purification Techniques	16
Development of Potent and Selective Janus Kinase 2/3 Directing PG–PROTACs	16
Discovery of TDI-10229: A Potent and Orally Bioavailable Inhibitor of Soluble Adenylyl Cyclase (sAC, ADCY10)	16
Discovery of Small Molecule Entry Inhibitors Targeting the Fusion Peptide of SARS-CoV-2 Spike Protein	16
Discovery of Tricyclic Xanthines as Agonists of the Cannabinoid-Activated Orphan G-Protein-Coupled Receptor GPR18	16
Dioxane-Linked Amide Derivatives as Novel Bacterial Topoisomerase Inhibitors against Gram-Positive Staphylococcus aureus	16
Promising Non-cytotoxic Monosubstituted Chalcones to Target Monoamine Oxidase-B	16
From Bacteria to Cancer: A Benzothiazole-Based DNA Gyrase B Inhibitor Redesigned for Hsp90 C-Terminal Inhibition	16
Challenges and Opportunities for Drug Discovery in Developing Countries: The Example of Cutaneous Leishmaniasis	16
Identification of Potent Reverse Indazole Inhibitors for HPK1	16
Physicochemistry of Cereblon Modulating Drugs Determines Pharmacokinetics and Disposition	16
Thiophene-Pyrazolourea Derivatives as Potent, Orally Bioavailable, and Isoform-Selective JNK3 Inhibitors	15
Toward the Target: Tilorone, Quinacrine, and Pyronaridine Bind to Ebola Virus Glycoprotein	15
Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead	15
Rapid Evaluation of Small Molecule Cellular Target Engagement with a Luminescent Thermal Shift Assay	15
mRNA Display Reaches for the Clinic with New PCSK9 Inhibitor	15
Synthesis, Biological Evaluation, and Molecular Docking of Arylpyridines as Antiproliferative Agent Targeting Tubulin	15
Amide Tethered 4-Aminoquinoline-naphthalimide Hybrids: A New Class of Possible Dual Function Antiplasmodials	15
DNA-Encoded Library Hit Confirmation: Bridging the Gap Between On-DNA and Off-DNA Chemistry	14
Structural Basis for Targeting the Folded P-Loop Conformation of c-MET	14
Synthesis of C6-Substituted Purine Nucleoside Analogues via Late-Stage Photoredox/Nickel Dual Catalytic Cross-Coupling	14
Virtual Screening for Ligand Discovery at the σ1 Receptor	14
Computer Prediction of pKa Values in Small Molecules and Proteins	14
Design and Synthesis of 1,2-Deoxy-pyranose Derivatives of Spliceostatin A toward Prostate Cancer Treatment	14
Advancing New Chemical Modalities into Clinical Studies	14
Discovery and Development of Cyclic Peptide Inhibitors of CIB1	14
Discovery of a First-in-Class Inhibitor of the Histone Methyltransferase SETD2 Suitable for Preclinical Studies	14
Carbamate and N-Pyrimidine Mitigate Amide Hydrolysis: Structure-Based Drug Design of Tetrahydroquinoline IDO1 Inhibitors	14
Synthesis, Inhibitory Activity, and In Silico Modeling of Selective COX-1 Inhibitors with a Quinazoline Core	14
A Chemical Probe for the Methyl Transferase PRMT5 with a Novel Binding Mode	14
meso-Thiophenium Porphyrins and Their Zn(II) Complexes: A New Category of Cationic Photosensitizers	13
Thiol- and Disulfide-Containing Vancomycin Derivatives Against Bacterial Resistance and Biofilm Formation	13
Antivirals against (Re)emerging Flaviviruses: Should We Target the Virus or the Host?	13
Site-specific Incorporation of 2′,5′-Linked Nucleic Acids Enhances Therapeutic Profile of Antisense Oligonucleotides	13
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity	13
Brain Penetrable Inhibitors of Ceramide Galactosyltransferase for the Treatment of Lysosomal Storage Disorders	13
Discovery of Vixotrigine: A Novel Use-Dependent Sodium Channel Blocker for the Treatment of Trigeminal Neuralgia	13
Hepatoselective Dihydroquinolizinone Bis-acids for HBsAg mRNA Degradation	13
Ugi Reaction Synthesis of Oxindole–Lactam Hybrids as Selective Butyrylcholinesterase Inhibitors	13
Sweet and Blind Spots in E3 Ligase Ligand Space Revealed by a Thermophoresis-Based Assay	13
New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes	13
Synthesis of Novel Ciprofloxacin-Based Hybrid Molecules toward Potent Antimalarial Activity	13
Discovery of DS79932728: A Potent, Orally Available G9a/GLP Inhibitor for Treating β-Thalassemia and Sickle Cell Disease	13
Bromocriptine as a Novel Pharmacological Chaperone for Mucopolysaccharidosis IV A	13
Dual Reversible Coumarin Inhibitors Mutually Bound to Monoamine Oxidase B and Acetylcholinesterase Crystal Structures	13
Discovery of RO7185876, a Highly Potent γ-Secretase Modulator (GSM) as a Potential Treatment for Alzheimer’s Disease	13
A Green-Absorbing, Red-Fluorescent Phenalenone-Based Photosensitizer as a Theranostic Agent for Photodynamic Therapy	13
1,5-Disubstituted 1,2,3-Triazoles as Amide Bond Isosteres Yield Novel Tumor-Targeting Minigastrin Analogs	12
Design and Synthesis of TRAP1 Selective Inhibitors: H-Bonding with Asn171 Residue in TRAP1 Increases Paralog Selectivity	12
Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448)	12
Novel Copper(II) Complex with a 4-Acylpyrazolone Derivative and Coligand Induce Apoptosis in Liver Cancer Cells	12
Structural Basis for Activation of Human Sirtuin 6 by Fluvastatin	12
Bisubstrate Inhibitors of Severe Acute Respiratory Syndrome Coronavirus-2 Nsp14 Methyltransferase	12
Synthesis and Evaluation of Ginkgolic Acid Derivatives as SUMOylation Inhibitors	12
Conjugation of a Blood Brain Barrier Peptide Shuttle to an Fc Domain for Brain Delivery of Therapeutic Biomolecules	12
Bioisostere Effects on the EPSA of Common Permeability-Limiting Groups	12
Semisynthetic Analogs of the Antibiotic Fidaxomicin—Design, Synthesis, and Biological Evaluation	12
Conversion of a PROTAC Mutant Huntingtin Degrader into Small-Molecule Hydrophobic Tags Focusing on Drug-like Properties	12
Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity	12

Fueling the Pipeline via Innovations in Organic Synthesis	12
Discovery of a Series of Pyrazinone RORγ Antagonists and Identification of the Clinical Candidate BI 730357	12
Discovery of Potent and Selective 7-Azaindole Isoindolinone-Based PI3Kγ Inhibitors	12
Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening Approach	12
Role of Fluorination in the Histone Deacetylase 6 (HDAC6) Selectivity of Benzohydroxamate-Based Inhibitors	12
SJPYT-195: A Designed Nuclear Receptor Degrader That Functions as a Molecular Glue Degrader of GSPT1	12
Contemporary Progress and Opportunities in RNA-Targeted Drug Discovery	11
Conjugation Ratio, Light Dose, and pH Affect the Stability of Panitumumab–IR700 for Near-Infrared Photoimmunotherapy	11
Indole-Containing Pyrazino[2,1-b]quinazoline-3,6-diones Active against Plasmodium and Trypanosomatids	11
Novel Blocker of Onco SK3 Channels Derived from Scorpion Toxin Tamapin and Active against Migration of Cancer Cells	11
Selective DYRK1A Inhibitor for the Treatment of Neurodegenerative Diseases: Alzheimer, Parkinson, Huntington, and Down Syndrome	11
Semisynthetic Derivatives of the Verticillin Class of Natural Products through Acylation of the C11 Hydroxy Group	11
Targeted Covalent Inhibition of Plasmodium FK506 Binding Protein 35	11
Sulfamoylbenzamide-based Capsid Assembly Modulators for Selective Inhibition of Hepatitis B Viral Replication	11
Structure-Based Discovery of Proline-Derived Arginase Inhibitors with Improved Oral Bioavailability for Immuno-Oncology	11
Automation of Synthesis in Medicinal Chemistry: Progress and Challenges	11
Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction	11
Synthesis of HDAC Inhibitor Libraries via Microscale Workflow	11
Discovery of Small-Molecule CD33 Pre-mRNA Splicing Modulators	11
Novel Thienopyridines as RIPK2 Inhibitors for Treating Inflammatory Bowel Disease	11
Studying Histone Deacetylase Inhibition and Apoptosis Induction of Psammaplin A Monomers with Modified Thiol Group	11
Novel Nitrile Peptidomimetics for Treating COVID-19	11
Structural Basis of Inhibition of Insulin-Regulated Aminopeptidase by a Macrocyclic Peptidic Inhibitor	11
Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma	11
BRD9 Bifunctional Degraders for Treating Cancer	11
Biological Evaluation of 5′-(N-Ethylcarboxamido)adenosine Analogues as Grp94-Selective Inhibitors	11
Design, Synthesis, and Evaluation of PD-1/PD-L1 Antagonists Bearing a Benzamide Scaffold	11
Discovery of Antibacterial Contezolid Acefosamil: Innovative O-Acyl Phosphoramidate Prodrug for IV and Oral Therapies	11
Optimization of Versatile Oxindoles as Selective PI3Kδ Inhibitors	11
Discovery of Adamantane Carboxamides as Ebola Virus Cell Entry and Glycoprotein Inhibitors	11
Discovery of Surfactins as Inhibitors of MicroRNA Processing Using Cat-ELCCA	11
Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors	11
Polysaccharide-Based Nanoparticles for Two-Step Responsive Release of Antitumor Drug	11
The Basicity Makes the Difference: Improved Canavanine-Derived Inhibitors of the Proprotein Convertase Furin	11
N-Aromatic-Substituted Indazole Derivatives as Brain-Penetrant and Orally Bioavailable JNK3 Inhibitors	11
Identification of Inhibitors of Thrombospondin 1 Activation of TGF-β	11
Novel Small Molecule RNA m6A Demethylase AlkBH5 Inhibitors for Treating Cancer	10
Amide–Amine Replacement in Indole-2-carboxamides Yields Potent Mycobactericidal Agents with Improved Water Solubility	10
Escaping from Flatland: Antimalarial Activity of sp3-Rich Bridged Pyrrolidine Derivatives	10
Antitubercular Activity of Novel 2-(Quinoline-4-yloxy)acetamides with Improved Drug-Like Properties	10
Triazine-Based Covalent DNA-Encoded Libraries for Discovery of Covalent Inhibitors of Target Proteins	10
A Retrospective Look at the Impact of Binding Site Environment on the Optimization of TRPA1 Antagonists	10
Flavonol-Based Carbon Monoxide Delivery Molecule with Endoplasmic Reticulum, Mitochondria, And Lysosome Localization	10
Structure–Activity Relationship and In Silico Evaluation of cis- and trans-PCPA-Derived Inhibitors of LSD1 and LSD2	10
Relevance of the Trillion-Sized Chemical Space “eXplore” as a Source for Drug Discovery	10
Structure-based Discovery of Cell-Potent Peptidomimetic Inhibitors for Protein N-Terminal Methyltransferase 1	10
Discovery of Potent Inhibitors of Streptococcus mutans Biofilm with Antivirulence Activity	10
2-Trifluoromethylthiazole-5-carboxamides: Analogues of a Stilbene-Based Anti-HIV Agent that Impact HIV mRNA Processing	10
Large-Scale Screening of Antifungal Peptides Based on Quantitative Structure–Activity Relationship	10
Dual-Target Inhibitors of the Folate Pathway Inhibit Intrinsically Trimethoprim-Resistant DfrB Dihydrofolate Reductases	10
Vinyl Sulfone-Based Inhibitors of Nonstructural Protein 2 Block the Replication of Venezuelan Equine Encephalitis Virus	10
Fluorescent Probes for Ecto-5′-nucleotidase (CD73)	10
Hydrophobic Tagging-Induced Degradation of PDEδ in Colon Cancer Cells	10
SMARCA2/4 PROTAC for Targeted Protein Degradation and Cancer Therapy	10
Discovery of 2,4-1H-Imidazole Carboxamides as Potent and Selective TAK1 Inhibitors	10
In Silico Targeting of the Long Noncoding RNA MALAT1	10
Covalent Bridging of Corilagin Improves Antiferroptosis Activity: Comparison with 1,3,6-Tri-O-galloyl-β-d-glucopyranose	10
Accelerating Drug Discovery: Synthesis of Complex Chemotypes via Multicomponent Reactions	10
A New Highly Deuterated [18F]AV-45, [18F]D15FSP, for Imaging β-Amyloid Plaques in the Brain	10
Novel Isoindolinone-Based Analogs of the Natural Cyclic Peptide Fenestin A: Synthesis and Antitumor Activity	10
Macrocyclic Peptides as a Novel Class of NNMT Inhibitors: A SAR Study Aimed at Inhibitory Activity in the Cell	10
Mining Public Domain Data to Develop Selective DYRK1A Inhibitors	10
A Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors	10
Novel Histone Deacetylase 6 Inhibitors for Treating Alzheimer’s Disease and Cancer	10
Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity	10
Dual Glycolate Oxidase/Lactate Dehydrogenase A Inhibitors for Primary Hyperoxaluria	10
Discovery of a Potent and Selective Covalent p300/CBP Inhibitor	10
Novel Histone Acetyltransferase (HAT) Inhibitors for Treating Diseases	10
Virtual Screening Approach to Identifying a Novel and Tractable Series of Pseudomonas aeruginosa Elastase Inhibitors	10
The Compelling Demand for an Effective PrPC-Directed Therapy against Prion Diseases	10
Discovery of Imidazopyridines as Potent Inhibitors of Indoleamine 2,3-Dioxygenase 1 for Cancer Immunotherapy	9
Synthesis and Evaluation of Neutral Phosphate Triester Backbone-Modified siRNAs	9
Structure–Activity Study of Nitazoxanide Derivatives as Novel STAT3 Pathway Inhibitors	9
Benzoxazepine-Derived Selective, Orally Bioavailable Inhibitor of Human Acidic Mammalian Chitinase	9
Discovery of Arylsulfonamide Nav1.7 Inhibitors: IVIVC, MPO Methods, and Optimization of Selectivity Profile	9
Identification of Novel Rho-Kinase-II Inhibitors with Vasodilatory Activity	9
Substituted 2,3-Benzodiazepines Derivatives as Bromodomain BRD4 Inhibitors	9
Discovery of Orally Active and Nonsteroidal Farnesoid X Receptor (FXR) Antagonist with Propensity for Accumulation and Responsiveness in Ileum	9
Lathyrane Diterpenoids as Novel hPXR Agonists: Isolation, Structural Modification, and Structure–Activity Relationships	9
Efficient NMR Screening Approach to Discover Small Molecule Fragments Binding Structured RNA	9
Discovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3Kγ Inhibitors	9
Discovery of a Pyrimidothiazolodiazepinone as a Potent and Selective Focal Adhesion Kinase (FAK) Inhibitor	9
Comprehensive Strategies to Bicyclic Prolines: Applications in the Synthesis of Potent Arginase Inhibitors	9
Derivatization Design of Synthetically Accessible Space for Optimization: In Silico Synthesis vs Deep Generative Design	9
Novel Dithiolane-Based Ligands Combining Sigma and NMDA Receptor Interactions as Potential Neuroprotective Agents	9
Sigma Receptor Ligands Carrying a Nitric Oxide Donor Nitrate Moiety: Synthesis, In Silico, and Biological Evaluation	9
Synthesis, Anti-Plasmodial Activities, and Mechanistic Insights of 4-Aminoquinoline-Triazolopyrimidine Hybrids	9
Structure-Based Design of A-1293102, a Potent and Selective BCL-XL Inhibitor	9
Investigation on the Anticancer Activity of Symmetric and Unsymmetric Cyclic Sulfamides	9
Scaffold Repurposing of in-House Chemical Library toward the Identification of New Casein Kinase 1 δ Inhibitors	9
Monocyclic Nitro-heteroaryl Nitrones with Dual Mechanism of Activation: Synthesis and Antileishmanial Activity	9
Exploration of a 14-3-3 PPI Pocket by Covalent Fragments as Stabilizers	9
Discovery of Futibatinib: The First Covalent FGFR Kinase Inhibitor in Clinical Use	9
Design and Synthesis of Tranylcypromine-Derived LSD1 Inhibitors with Improved hERG and Microsomal Stability Profiles	9
Novel 2-Aryloxazoline Compounds Exhibit an Inhibitory Effect on Candida spp., Including Antifungal-Resistant Isolates	9