| Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers |
45 |
| Synthesis and Biological Screening of Pyrano[2-c]quinoline Analogues as Anti-inflammatory and Anticancer Agents |
21 |
| Harnessing Polypharmacology with Medicinal Chemistry |
20 |
| De Novo Discovery of Nonstandard Macrocyclic Peptides as Noncompetitive Inhibitors of the Zika Virus NS2B-NS3 Protease |
19 |
| Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity |
17 |
| LLY- a Potent and Selective Inhibitor of Arginine Methyltransferase PRMT with Antitumor Activity |
17 |
| Targeting IRAK4 for Degradation with PROTACs |
17 |
| What Do You Get from DNA-Encoded Libraries? |
16 |
| Carbon Dots from Sugars and Ascorbic Acid: Role of the Precursors on Morphology, Properties, Toxicity, and Drug Uptake |
16 |
| Replaceinent of the Thiosugar of Auranofin with Iodide Enhances the Anticancer Potency in a Mouse Model of Ovarian Cancer |
16 |
| Meridianin D Analogues Display Antibiofilm Activity against MRSA and Increase Colistin Efficacy in Gram-Negative Bacteria |
16 |
| Structure-Based Virtual Screening for the Discovery of Novel Inhibitors of New Delhi Metallo-beta-lactamase-1 |
15 |
| In Vivo Anticancer Activity of a Rhenium(I) Tricarbonyl Complex |
15 |
| Synthesis of Thymoquinone-Artemisinin Hybrids: New Potent Antileukemia, Antiviral, and Antimalarial Agents |
15 |
| High in Vitro and in Vivo Tumor-Selective Novel Ruthenium(II) Complexes with 3-(2 '-Benzimidazolyl)-7-fluoro-coumarin |
14 |
| X-ray Crystallography Deciphers the Activity of Broad-Spectrum Boronic Acid beta-Lactamase Inhibitors |
13 |
| Dual GSK-3 beta/AChE Inhibitors as a New Strategy for Multitargeting Anti -Alzheimer's Disease Drug Discovery |
13 |
| Data Sets Representative of the Structures and Experimental Properties of FDA-Approved Drugs |
13 |
| Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8 |
12 |
| Maximizing ER-alpha Degradation Maximizes Activity in a Tamoxifen-Resistant Breast Cancer Model: Identification of GDC-0927 |
12 |
| Identification and Structure-Guided Development of Pyrimidinone Based USP7 Inhibitors |
12 |
| Discovery of Novel Indoleamine 3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors |
12 |
| The ProTide Prodrug Technology: Where Next? |
11 |
| Targeting Tumor Associated Carbonic Anhydrases IX and XII: Highly Isozyme Selective Coumarin and Psoralen Inhibitors |
11 |
| Biocompatible Boron-Containing Prodrugs of Belinostat for the Potential Treatment of Solid Tumors |
11 |
| Aminoisoxazoles as Potent Inhibitors of Tryptophan 3-Dioxygenase 2 (TDO2) |
11 |
| Improved Selective Class I HDAC and Novel Selective HDAC3 Inhibitors: Beyond Hydroxamic Acids and Benzamides |
10 |
| Chalcones and Chalcone-mimetic Derivatives as Notch Inhibitors in a Model of T-cell Acute Lymphoblastic Leukemia |
10 |
| Discovery of N-(1-Acryloylazetidin-3-yl)-2-(1H-indol-1-yl)acetamides as Covalent Inhibitors of KRAS(G12C) |
10 |
| Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yI)sulfones as Selective, Orally Active ROR gamma t Inverse Agonists |
10 |
| Profiling and Application of Photoredox C(sp(3))-C(sp(2)) Cross-Coupling in Medicinal Chemistry |
10 |
| Discovery of Amino-cyclobutarene-derived Indoleamine-3-dioxygenase 1 (IDO1) Inhibitors for Cancer Immunotherapy |
10 |
| Escaping from Flatland: [2+2] Photocycloaddition; Conformationally Constrained sp(3)-rich Scaffolds for Lead Generation |
10 |
| 2-Formylpyridyl Ureas as Highly Selective Reversible-Covalent Inhibitors of Fibroblast Growth Factor Receptor 4 |
10 |
| Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer |
10 |
| In Silico Identification of Piperidinyl-amine Derivatives as Novel Dual Binders of Oncogene c-myc/c-Kit G-quadruplexes |
9 |
| Closing the Loop: Developing an Integrated Design, Make, and Test Platform for Discovery |
9 |
| Rhodanine as a Potent Scaffold for the Development of Broad Spectrum Metallo-beta-lactamase inhibitors |
9 |
| Evaluating the Advantages of Using 3D-Enriched Fragments for Targeting BET Bromodomains |
9 |
| Discovery of the First-in-Class GSK-3 beta/HDAC Dual Inhibitor as Disease-Modifying Agent To Combat Alzheimer's Disease |
9 |
| H2O2/Peroxynitrite-Activated Hydroxamic Acid HDAC Inhibitor Prodrugs Show Antileukemic Activities against AML Cells |
9 |
| Novel Nitric Oxide Donors of Phenylsulfonylfuroxan and 3-Benzyl Coumarin Derivatives as Potent Antitumor Agents |
9 |
| Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery |
9 |
| Synthesis of Artemisinin-Estrogen Hybrids Highly Active against HCMV, P-falciparum, and Cervical and Breast Cancer |
9 |
| Expansion of cat-ELCCA for the Discovery of Small Molecule Inhibitors of the Pre-let-7-Lin28 RNA-Protein Interaction |
8 |
| Discovery of Spiro Oxazolidinediones as Selective, Orally Bioavailable Inhibitors of p300/CBP Histone Acetyltransferases |
8 |
| Prediction of Drug-Target Binding Kinetics by Comparative Binding Energy Analysis |
8 |
| High-Resolution Crystal Structure of Endoplasmic Reticulum Aminopeptidase 1 with Bound Phosphinic Transition-State Analogue Inhibitor |
8 |
| Exploiting Chemical Toolboxes for the Expedited Generation of Tetracyclic Quinolines as a Novel Class of PXR Agonists |
8 |
| Restoring Let-7 microRNA Biogenesis Using a Small-Molecule Inhibitor of the Protein-RNA Interaction |
8 |
