| Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design |
220 |
| The Current State of Peptide Drug Discovery: Back to the Future? |
121 |
| Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones? |
78 |
| Ru(II) Compounds: Next-Generation Anticancer Metallotherapeutics? |
65 |
| Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology |
62 |
| Polypharmacology by Design: A Medicinal Chemist's Perspective on Multitargeting Compounds |
60 |
| Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression |
52 |
| Nitro-Group-Containing Drugs |
51 |
| Two Decades under the Influence of the Rule of Five and the Changing Properties of Approved Oral Drugs |
50 |
| Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer |
47 |
| Applications of Deuterium in Medicinal Chemistry |
47 |
| Discovery of Risdiplam, a Selective Survival of Motor Neuron-2 (SMN2) Gene Splicing Modifier for the Treatment of Spinal Muscular Atrophy (SMA) |
43 |
| Emerging Trends in Flow Chemistry and Applications to the Pharmaceutical Industry |
43 |
| Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1 |
42 |
| Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals) |
42 |
| Discovery and Characterization of AZD a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent |
41 |
| Beyond the Rule of 5: Lessons Learned from AbbVie's Drugs and Compound Collection |
41 |
| Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression |
40 |
| Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel-Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7 |
40 |
| Carbon Monoxide and Its Controlled Release: Therapeutic Application, Detection, and Development of Carbon Monoxide Releasing Molecules (CORMs) |
39 |
| Modulators of 14-3-3 Protein-Protein Interactions |
39 |
| Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER) |
38 |
| Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds |
38 |
| Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression |
37 |
| Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-beta-Lactamases |
37 |
| Inhibit or Evade Multidrug Resistance P-Glycoprotein in Cancer Treatment |
36 |
| From Oxiranes to Oligomers: Architectures of US FDA Approved Pharmaceuticals Containing Oxygen Heterocycles |
35 |
| Polymethine Thiopyrylium Fluorophores with Absorption beyond 1000 nm for Biological Imaging in the Second Near-Infrared Subwindow |
34 |
| A Survey of the Structures of US FDA Approved Combination Drugs |
34 |
| Inhibitors of Melanogenesis: An Updated Review |
31 |
| Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1 |
30 |
| Lipophilic Efficiency as an Important Metric in Drug Design |
29 |
| Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development |
29 |
| Medical Uses of Silver: History, Myths, and Scientific Evidence |
29 |
| Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK) |
29 |
| Ligand-Based Fluorine NMR Screening: Principles and Applications in Drug Discovery Projects |
29 |
| Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase |
28 |
| Antibiotic Adjuvants: Make Antibiotics Great Again! |
28 |
| The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic |
28 |
| Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy |
28 |
| A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos |
27 |
| Allosteric Modulator Discovery: From Serendipity to Structure-Based Design |
27 |
| Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update |
27 |
| Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms |
26 |
| Virtual Chemical Libraries Miniperspective |
26 |
| Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity |
26 |
| The ProTide Prodrug Technology: From the Concept to the Clinic |
26 |
| Discovery of Novel Quinoline-Chalcone Derivatives as Potent Antitumor Agents with Microtubule Polymerization Inhibitory Activity |
25 |
| Targeting Multiple Effector Pathways in Pancreatic Ductal Adenocarcinoma with a G-Quadruplex-Binding Small Molecule |
25 |
| CF2H, a Functional Group-Dependent Hydrogen-Bond Donor: Is It a More or Less Lipophilic Bioisostere of OH, SH, and CH3? |
25 |