Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions

Hard and Soft Acids and Bases

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New Substructure Filters for Removal of Pan Assay Interference Compounds (PAINS) from Screening Libraries and for Their Exclusion in Bioassays

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Therapeutic potential of resveratrol: the in vivo evidence

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AZD9291, an Irreversible EGFR TKI, Overcomes T790M-Mediated Resistance to EGFR Inhibitors in Lung Cancer

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The resurgence of covalent drugs

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Prodrugs: design and clinical applications

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Covalent binding design strategy: A prospective method for discovery of potent targeted anticancer agents

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Cytotoxicity and Pro-/Anti-inflammatory Properties of Cinnamates, Acrylates and Methacrylates Against RAW264.7 Cells

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Spirocyclizations Involving Oxonium Ylides Derived from Cyclic α-Diazocarbonyl Compounds: An Entry into 6-Oxa-2-azaspiro[4.5]decane Scaffold

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A chemical perspective on the modulation of TEAD transcriptional activities: Recent progress, challenges, and opportunities

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Identification of a diverse synthetic abietane diterpenoid library and insight into the structure-activity relationships for antibacterial activity

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Asymmetric FeII-Catalyzed Thia-Michael Addition Reaction to α,β-Unsaturated Oxazolidin-2-one Derivatives

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Novel Curcumin Inspired Bis-Chalcone Promotes Endoplasmic Reticulum Stress and Glioblastoma Neurosphere Cell Death

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Gains from no real PAINS: Where ‘Fair Trial Strategy’ stands in the development of multi-target ligands

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Modeling the Binding and Conformational Energetics of a Targeted Covalent Inhibitor to Bruton’s Tyrosine Kinase

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Chemical inhibition of mitochondrial fission via targeting the DRP1-receptor interaction

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Tideglusib and Its Analogues As Inhibitors of Staphylococcus aureus SrtA

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Parthenolide Destabilizes Microtubules by Covalently Modifying Tubulin

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Late‐Stage C−H Activation of Drug (Derivative) Molecules with Pd(ll) Catalysis

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Molecular, chemical, and structural characterization of prostaglandin A2 as a novel agonist for Nur77

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Electrophilic Compounds in the Human Diet and Their Role in the Induction of the Transcription Factor NRF2

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Butoxy Mansonone G Inhibits STAT3 and Akt Signaling Pathways in Non-Small Cell Lung Cancers: Combined Experimental and Theoretical Investigations

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Synthesis and structure-activity relationships of new chiral spiro-β-lactams highly active against HIV-1 and Plasmodium

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Covalent chemical probes for protein kinases

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Terminators or Guardians? Design, Synthesis, and Cytotoxicity Profiling of Chalcone-Sulfonamide Hybrids

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Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyridazinone derivatives as covalent FGFR inhibitors

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N-Terminal cysteine mediated backbone-side chain cyclization for chemically enhanced phage display

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Mechanistic aspects of thiol additions to Michael acceptors: Insights from computations

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Allenamide as a bioisostere of acrylamide in the design and synthesis of targeted covalent inhibitors

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Covalent allosteric modulation: An emerging strategy for GPCRs drug discovery

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Polyphenols as adjunctive treatments in psychiatric and neurodegenerative disorders: Efficacy, mechanisms of action, and factors influencing inter-individual response

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Dehydropeptide Supramolecular Hydrogels and Nanostructures as Potential Peptidomimetic Biomedical Materials

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Reversible covalent c-Jun N-terminal kinase inhibitors targeting a specific cysteine by precision-guided Michael-acceptor warheads

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Photopolymerized Starchstarch Nanoparticle (SNP) network hydrogels

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A novel TLR7 agonist as adjuvant to stimulate high quality HBsAg-specific immune responses in an HBV mouse model

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CeO2-Supported Pd(II)-on-Au Nanoparticle Catalyst for Aerobic Selective α,β-Desaturation of Carbonyl Compounds Applicable to Cyclohexanones

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Targeting eukaryotic proteases for natural products-based drug development

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The Natural Products Withaferin A and Withanone from the Medicinal HerbWithania somniferaAre Covalent Inhibitors of the SARS-CoV-2 Main Protease

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Covalent hits and where to find them

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Catalytic Asymmetric [4+2]‐Cycloadditions Using Tropolones: Developments, Scope, Transformations, and Bioactivity

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Pharmacophore-Directed Retrosynthesis Applied to Rameswaralide: Synthesis and Bioactivity of Sinularia Natural Product Tricyclic Cores

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Targeted Covalent Inhibition of Telomerase

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Reactive Sulfur Species and Protein Persulfidation: An Emerging Redox Axis in Human Health and Disease

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Determination of Protein Haptenation by Chemical Sensitizers Within the Complexity of the Human Skin Proteome

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Spiralyde A, an Antikinetoplastid Dolabellane from the Brown Alga Dictyota spiralis

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Development of catalyst-free carbon-sulfur bond formation reactions under aqueous media and their applications

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Reactivity-directed analysis – a novel approach for the identification of toxic organic electrophiles in drinking water

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Into the Fray! A Beginner's Guide to Medicinal Chemistry

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Development of an 18F-Labeled Irreversible Inhibitor of Transglutaminase 2 as Radiometric Tool for Quantitative Expression Profiling in Cells and Tissues

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Sulfur in Dynamic Covalent Chemistry

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Synthesis of SARS-CoV-2 M pro inhibitors bearing a cinnamic ester warhead with in vitro activity against human coronaviruses

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Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective

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Synthesis of Acrylamides via the Doebner–Knoevenagel Condensation

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Synthesis and antimicrobial evaluation of new halogenated 1,3-Thiazolidin-4-ones

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From irreversible to reversible covalent inhibitors: Harnessing the andrographolide scaffold for anti-inflammatory action

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Synthesis, biological evaluation and X-ray crystallographic analysis of novel (E)-2-cyano-3-(het)arylacrylamides as potential anticancer agents

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Manganese(I) Catalyzed α-Alkenylation of Amides Using Alcohols with Liberation of Hydrogen and Water

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Discovery of Novel Celastrol–Imidazole Derivatives with Anticancer Activity In Vitro and In Vivo

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Covalent small-molecule inhibitors of SARS-CoV-2 Mpro: Insights into their design, classification, biological activity, and binding interactions

Shawky, A. M., Almalki, F. A., Alzahrani, H. A., Abdalla, A. N., Youssif, B. G. M., Ibrahim, N. A., Gamal, M., El-Sherief, H. A. M., Abdel‐Fattah, M. M., Hefny, A. A., et al. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116704 · Cited by 26

A one-pot metal-free protocol for the synthesis of chalcogenated furans from 1,4-enediones and thiols

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Anticancer properties of 5Z-(4-fluorobenzylidene)-2-(4-hydroxyphenylamino)-thiazol-4-one

Szychowski, K. A., Kaminskyy, D. V., Leja, M. L., Kryshchyshyn‐Dylevych, A., Lesyk, R., Tobiasz, J., Wnuk, M., Pomianek, T., & Gmiński, J. (2019) · Scientific Reports · doi:10.1038/s41598-019-47177-6 · Cited by 26

Discovery of a Natural Product That Binds to the Mycobacterium tuberculosis Protein Rv1466 Using Native Mass Spectrometry

Elnaas, A. R., Grice, I. D., Han, J., Feng, Y., Capua, A. D., Mak, T., Laureanti, J. A., Buchko, G. W., Myler, P. J., Cook, G. M., et al. (2020) · Molecules · doi:10.3390/molecules25102384 · Cited by 26

Benzylideneacetone Derivatives Inhibit Osteoclastogenesis and Activate Osteoblastogenesis Independently Based on Specific Structure–Activity Relationship

Pativada, T., Kim, M. H., Lee, J.-H., Hong, S. S., Choi, C. W., Choi, Y., Kim, W. J., Song, D.-W., Park, S. I., Lee, E. J., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00270 · Cited by 25

Targeted Covalent Inhibition of Plasmodium FK506 Binding Protein 35

Atack, T. C., Raymond, D. D., Blomquist, C., Pasaje, C. F. A., McCarren, P. R., Moroco, J. A., Befekadu, H. B., Robinson, F. P., Pal, D., Esherick, L. Y., et al. (2020) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.0c00272 · Cited by 25

Exploration of BAY 11-7082 as a Potential Antibiotic

Coles, V. E., Darveau, P., Zhang, X., Harvey, H., Henriksbo, B. D., Yang, A., Schertzer, J. D., Magolan, J., & Burrows, L. L. (2021) · ACS Infectious Diseases · doi:10.1021/acsinfecdis.1c00522 · Cited by 25

Helenalin Analogues Targeting NF‐κB p65: Thiol Reactivity and Cellular Potency Studies of Varied Electrophiles

Widen, J. C., Kempema, A., Baur, J. W., Skopec, H. M., Edwards, J. T., Brown, T. J., Brown, D. A., Meece, F. A., & Harki, D. A. (2018) · ChemMedChem · doi:10.1002/cmdc.201700752 · Cited by 25

Bioactive Resorcylic Acid Lactones with Different Ring Systems from Desert Plant Endophytic Fungus Chaetosphaeronema hispidulur

Zhang, X., Liu, Z., Sun, B., Niu, S., Wang, M.-H., Tan, X., Zou, Z.-M., & Ding, G. (2018) · Journal of Agricultural and Food Chemistry · doi:10.1021/acs.jafc.8b02648 · Cited by 25

The McKenna reaction – avoiding side reactions in phosphonate deprotection

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Reaction of Chalcones with Cellular Thiols. The Effect of the 4-Substitution of Chalcones and Protonation State of the Thiols on the Addition Process. Diastereoselective Thiol Addition

Kenari, F., Molnár, S., & Perjési, P. (2021) · Molecules · doi:10.3390/molecules26144332 · Cited by 25

Activatable covalent labeling probes: design, mechanism, and biological applications

Miao, Y., Tian, Y., & Ye, D. (2025) · Chemical Society Reviews · doi:10.1039/d5cs00984g · Cited by 24

Discovery of novel allosteric site and covalent inhibitors of FBPase with potent hypoglycemic effects

Huang, Y., Wei, L., Han, X., Chen, H., Ren, Y., Xu, Y., Song, R., Rao, L., Chen, S., Peng, C., et al. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2019.111749 · Cited by 24

Itaconic acid hybrids as potential anticancer agents

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Chemistry and biology of enzymes in protein glutathionylation

Oppong, D., Schiff, W., Shivamadhu, M. C., & Ahn, Y. (2023) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2023.102326 · Cited by 24

Covalent Kinase Inhibitors: An Overview

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Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity

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Electrophilic Natural Products as Drug Discovery Tools

Gehrtz, P., & London, N. (2021) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2021.03.008 · Cited by 25

Structure-Based Design of N -(5-Phenylthiazol-2-yl)acrylamides as Novel and Potent Glutathione S-Transferase Omega 1 Inhibitors

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A Stereoselective, Multicomponent Catalytic Carbonylative Approach to a New Class of α,β-Unsaturated γ-Lactam Derivatives

Mancuso, R., Ziccarelli, I., Brindisi, M., Altomare, C., Frattaruolo, L., Falcicchio, A., Ca’, N. D., Cappello, A. R., & Gabriele, B. (2021) · Catalysts · doi:10.3390/catal11020227 · Cited by 23

Nucleophilic Reactivities of Thiophenolates

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Rapid Access to Multisubstituted Acrylamides from Cyclic Ketones via Palladium/Norbornene Cooperative Catalysis

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Identification of structural features of selected flavonoids responsible for neuroprotection using a Drosophila model of Parkinson’s disease

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Synthesis of Diverse N-Acryloyl Azetidines and Evaluation of Their Enhanced Thiol Reactivities

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Stereoselective total synthesis of parthenolides indicates target selectivity for tubulin carboxypeptidase activity

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