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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Absolute hardness: companion parameter to absolute electronegativity

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Electrophilicity Index

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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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Density functional approach to the frontier-electron theory of chemical reactivity

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Hard and soft acids and bases, HSAB, part 1: Fundamental principles

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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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Triazole and Pyrazole Hybrids of Electrophilic Natural Products as Promising Anticancer Agents

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Discovery of chalcone derivatives as antileishmanial agents: phenotypic screening, exploratory docking and enzymatic assays on trypanothione reductase and related flavoproteins

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Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries

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3,28-Diacetoxylup-20(29)-ene-30-oic Acid and Its ω-Bromoalkyl Esters

Ponomaryov, D. V., Grigor’eva, L. R., Nemtarev, A. V., Tsepaeva, O. V., Mironov, V. F., Gnezdilov, O. I., & Antipin, I. S. (2020) · Russian Journal of Organic Chemistry · doi:10.1134/s1070428020040107 · Cited by 3

N-Benzyl, N-phenethyl and N-benzyloxybenzamide derivatives inhibit amyloid-beta (Aβ42) aggregation and mitigate Aβ42-induced neurotoxicity

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4‐Aza Cyclopentenone Prostaglandin Analogues: Synthesis and NF‐κB Inhibitory Activities

Doherty, W., Conway, L., Leveau, B., Nacca, F. G., Chiappa, L., Riccio, A., Roberts, S. M., Santoro, M. G., & Evans, P. (2024) · ChemMedChem · doi:10.1002/cmdc.202400823 · Cited by 3

Covalent Epidermal Growth Factor Receptor (EGFR) Inhibitors in Targeted Therapy of Drug-Resistant Non-Small Cell Lung Cancer (A Review)

Shvetsov, A. B., & Semenov, A. (2024) · Russian Journal of Bioorganic Chemistry · doi:10.1134/s1068162024060347 · Cited by 3

A New Potential Atmospheric Accretion Mechanism: Acid-Catalyzed Hetero-Michael Addition Reactions

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Chebulinic acid shields Villin 1 from covalent attack to mitigate Euphorbia fischeriana enterotoxicity: A basis for safer anti-ascites therapy

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Mechanism study on asymmetric Michael addition reaction between alkynone and α-angelica lactone catalyzed by chiral N, N'-dioxide-Sc(III) complex

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Identification of rapid access to polycyclic systems via a base-catalyzed cascade cyclization reaction and their biological evaluation

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Synthesis of the 4-aza cyclopentenone analogue of Δ12,14-15-deoxy-PGJ2 and S-cysteine adducts

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Synthesis of Colibactin Pyrrolidono[3,4-d]pyridones via Regioselective C(sp3)–H Activation

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A Transient Initiator for Polypeptoids Postpolymerization α ‐Functionalization via Activation of a Thioester Group

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3, 3′-[succinylbis(diazaneyl)]bis(N,N,N-trimethylpropan-1-ammonium) perchlorate: Synthesis, characterization, computational studies and in vitro anticancer activity against the human colon carcinoma cell line (HT-29)

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Mutate and Conjugate: A Method to Enable Rapid In-Cell Target Validation

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Ionic-molecular organocatalysis enabling allylic amination reactions

Lokhande, S. K., Vaidya, G. N., Venkatesh, A., Patel, V. D., Joshi, P. K., Chatterjee, D. R., & Kumar, D. (2024) · Cell Reports Physical Science · doi:10.1016/j.xcrp.2024.101868 · Cited by 3

Discovery of Loureirin analogues with colorectal cancer suppressive activity via regulating cell cycle and Fas death receptor

Li, P., Tian, X., Zhang, D., Ou, H., Huang, Q., Jin, W., & Liu, R. (2024) · BMC Pharmacology and Toxicology · doi:10.1186/s40360-024-00758-2 · Cited by 3

Development of ketalized unsaturated saccharides as multifunctional cysteine-targeting covalent warheads

Dong, S., Huang, H. Y., Li, J., Li, X., Bunu, S. J., Yang, Y., Zhang, Y., Jia, Q., Xu, Z., Li, Y., et al. (2024) · Communications Chemistry · doi:10.1038/s42004-024-01279-z · Cited by 3

Synthesis, screening and validation of cysteine-reactive fragments as chikungunya virus protease inhibitors

He, J., Illingworth, H., Ullrich, S., Ghosh, P., Ton, J., Jackson, C. J., & Nitsche, C. (2025) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2025.130176 · Cited by 3

Michael addition–elimination–cyclization based turn-on fluorescence (MADELCY TOF) probes for cellular cysteine imaging and estimation of blood serum cysteine and aminoacylase-1

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TFA-mediated stereoselective aza-Michael addition for the synthesis of 3β-arylamine derivatives of withaferin A and evaluation of their anticancer potential

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Back to the Medicinal Chemistry Future

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Development of Chiral Bisphosphine Ligands with a Terminal Olefin Enables Asymmetric Orthogonal Auto‐Tandem Catalysis

He, D., Xu, H., Cao, P., Li, L., Luo, Y., Mon, E. E., Peng, F., Li, L., Dang, Y., & Shao, Z. (2025) · Angewandte Chemie · doi:10.1002/ange.202506881 · Cited by 2

Development of 9-cinnamyl-9H-purine derivatives as potent anticancer agents through inactivation of NF-κb/p65 and p-STAT1 signaling pathways: Discovery of a new template for adenosine receptor

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C2-Axis Chiral 10,10′-Bibenzoquinoline Ligands Specifically Partnered with AgOTf Enable Catalytic Enantioselective Cyclopropanations of Diazo Carbonates

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Programmable synthesis of alkaloidal frameworks integrating Michael acceptor generates covalent probes for targeting POLE3 in HBV replication

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Elucidation of a Novel Dual Binding Site on Tubulin: Theoretical Insights and Prospective Hybrid Inhibitors

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EGFR inhibitor-resistant lung cancers exhibit collateral sensitivity to a covalent, cysteine-independent KEAP1 oligomerizing molecular bridge

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Novel anticancer paeonol derivatives possessing a nitric oxide donor moiety as TrxR inhibitors: design, synthesis, biological evaluation

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Redirecting a Native Ene‐Reductase Toward Desaturation With Reverse Enantioselectivity

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Site-specific profiling of lysine itaconylation via a thiol-based probe

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Metal-Free C−H Aroylation of Alkenes Mediated by Triarylamine Visible-Light Photocatalysis

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

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Computer-Aided Design and Synthesis of (Functionalized quinazoline)–(α-substituted coumarin)–arylsulfonate Conjugates against Chikungunya Virus

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A thiol chemistry perspective on redox medicine

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Asymmetric Synthesis of α‐Methylene‐γ‐Butyrolactones via Tandem Allylboration/Lactonization: a Kinetic Resolution Process

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Synthesis of 9-Cinnamyl-9H-purine Derivatives as Novel TLR4/MyD88/NF-κB Pathway Inhibitors for Anti-inflammatory Effects

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Safety of ashitaba sap as a Novel food pursuant to Regulation (EU) 2015/2283

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Cinnamaldehyde alleviates hepatic steatosis correlating with its electrophilic capability

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An anti-mitotic compound, (+)-6-tuliposide A, isolated from the Canadian glacier lily, Erythronium grandiflorum

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A novel 1-benzoazepine-derived Michael acceptor and its hetero-adducts active against MRSA

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Unveiling a Novel Mechanistic Pathway: Thiol and DMSO ‐Facilitated Synthesis of Pyrazole Amine Thioether

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(E)-2-Benzylidenecyclanones: Part XX—Reaction of Cyclic Chalcone Analogs with Cellular Thiols: Unexpected Increased Reactivity of 4-Chromanone- Compared to 1-Tetralone Analogs in Thia-Michael Reactions

Bognár, G., Kenari, F., Pintér, Z., Borges, I. D., Camargo, A. J., de Oliveira, H. C. B., Sanches-Neto, F. O., Carvalho-Silva, V. H., Napolitano, H. B., & Perjési, P. (2024) · Molecules · doi:10.3390/molecules29235493 · Cited by 2

Investigation of Reactions Between Isothiazolinones and Cysteamine by Reactive Paper Spray Ionization Mass Spectrometry (Reactive PSI MS)

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Curcumin-cinnamaldehyde hybrids as antiproliferative agents against women’s cancer cells

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Optimized Asymmetric Synthesis of Umuravumbolide

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The Anti-Fungal Activity of Nitropropenyl Benzodioxole (NPBD), a Redox-Thiol Oxidant and Tyrosine Phosphatase Inhibitor

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Identifying new compounds active against Giardia duodenalis

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A Perspective on Covalent Inhibitors: Research and Development Trends of Warheads and TargetsPreprint

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Angelic Acid Prevents RANKL-Induced Osteoclastogenesis Through Pathway-Biased Inhibition of MAPK–NFATc1 SignalingPreprint

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Nucleophilie von Glutathion als Bindeglied zur Reaktivität von Michael‐Akzeptoren

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

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Nickel(II)‐Catalyzed Hydrocarbamoylation of Alkynes with Formamides towards Unsaturated Amides

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First fragment-based screening identifies new chemotypes inhibiting ERAP1-metalloprotease

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Capturing and releasing cucurbitacins with α, β-unsaturated group from Cucumis melo based on reversibility of thia-Michael addition reaction

Zhu, T., Hu, L., Hu, H., Li, Y., Zhu, J., Wu, G., & Xu, D. (2025) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2025.108404 · Cited by 1

Use of new approach methodology for hepatic safety assessment of covalent inhibitor drug candidates

Amberntsson, S., Foster, A. J., Chouhan, B., Wilkinson, S. D., Harlfinger, S., Smith, G., Kettle, J. G., Niedbala, M. J., Kavanagh, S. L., & Williams, D. P. (2025) · Toxicology Research · doi:10.1093/toxres/tfaf054 · Cited by 1

Thermolides D and E: Total Synthesis and Stereochemical Revision

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Unveiling the cytotoxicity of Red Sea Moorena producens via LC-QTOF-MS/MS chemical profiling, network pharmacology, and molecular docking

Abdelhady, E. M., Khalil, M. N. A., Rabeh, M. A., Alshehri, S. A., Sabry, O. M., & Hashem, M. M. (2025) · Pharmaceutical Biology · doi:10.1080/13880209.2025.2534573 · Cited by 1

Cinnamoylphenethyl amides from fissistigma bracteolatum and their anti-inflammatory activities

Xue, J., Jia, Y.-Y., Lei, J.-W., Sun, Y., Chen, H., Zhi, Y., Zhao, Z., Zhu, D., Li, G.-S., & Xue, G. (2025) · Natural Product Research · doi:10.1080/14786419.2025.2542256 · Cited by 1

Anemonin is one of two anti-mitotic activities present in extracts from the Canadian Prairie Crocus, Pulsatilla nuttalliana

Knibb, S. M. H., Lockwood, T. C., Yeremy, B., Molina, L., Beck, C. R., Sagoe-Wagner, A., Williams, D. E., Andersen, R. J., & Golsteyn, R. M. (2025) · Pharmacological Research - Natural Products · doi:10.1016/j.prenap.2025.100361 · Cited by 1

Electrophilic aryl migration of N -benzyl propiolamides to functionalized-acrylamides

Reddy, C. R., Vinaya, P. P., Ajaykumar, U., & Nagendraprasad, T. (2025) · Chemical Communications · doi:10.1039/d5cc04709a · Cited by 1

Modern Approaches to Anti-EGFR Therapy

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Targeting enzymes with covalent warheads: Beyond cysteine

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Cheke, R. S., & Kharkar, P. S. (2025) · Chemical Biology & Drug Design · doi:10.1111/cbdd.70211 · Cited by 1

Ecotoxicological Evaluation of Simple Xanthone, Cinnamic Acid, and Chalcone Derivatives Using the Microtox Assay for Sustainable Synthetic Design of Biologically Active Molecules

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Design of a Targeted Covalent Probe to Interrogate the DNA Polymerase Activity of Polθ

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Benzenoid ring C–H olefination of Coumarins under Rh(III)-catalysis: Synthesis, anti-inflammatory evaluation and in silico studies

Singh, A., Chopra, M., Mukherjee, A., Kamble, A., Jain, A., Kumar, H., & Sharma, S. (2026) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2026.109553 · Cited by 1

Modification of the dermal matrix by senescence associated lipids and its functional consequence

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Discovery of N -Ethyl Sulfonamide Derivatives as Potent Intestinal-Restricted Farnesoid X Receptor Antagonists for the Treatment of Metabolic Disorders

Su, L., Huo, T., Zhao, X., Pang, Z., Wang, T., Liu, Y., Dou, X., & Jiao, N. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c03064 · Cited by 1

Whole-Cell Biocatalysis for the Production of Structurally Diverse Methoxydihydrochalcones: Broad Activity of the Yarrowia Clade

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Angelic Acid Prevents RANKL-Induced Osteoclastogenesis Through Pathway-Biased Inhibition of MAPK–NFATc1 Signaling

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