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

Depurinating Acylfulvene−DNA Adducts: Characterizing Cellular Chemical Reactions of a Selective Antitumor Agent

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New Prostanoids with Cytotoxic Activity from Taiwanese Octocoral Clavularia viridis

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The Chemistry of Mycotoxins

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A Novel Acetylenic Tricyclic bis-(Cyano Enone) Potently Induces Phase 2 Cytoprotective Pathways and Blocks Liver Carcinogenesis Induced by Aflatoxin

Liby, K. T., Yore, M. M., Roebuck, B. D., Baumgartner, K. J., Honda, T., Sundararajan, C., Yoshizawa, H., Gribble, G. W., Williams, C. R., Risingsong, R., et al. (2008) · Cancer Research · doi:10.1158/0008-5472.can-08-1123 · Cited by 52

Iodine catalyzed conjugate addition of mercaptans to α,β-unsaturated carboxylic acids under solvent-free condition

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Lucidone protects human skin keratinocytes against free radical-induced oxidative damage and inflammation through the up-regulation of HO-1/Nrf2 antioxidant genes and down-regulation of NF-κB signaling pathway

Kumar, K. J. S., Yang, H., Tsai, Y.-C., Hung, P.-C., Chang, S.-H., Lo, H.-W., Shen, P.-C., Chen, S., Wang, H., Wang, S., et al. (2013) · Food and Chemical Toxicology · doi:10.1016/j.fct.2013.04.055 · Cited by 50

Equilibrium reactions of n-butanethiol with some conjugated heteroenoid compounds

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Differential selectivity of protein modification by the cyclopentenone prostaglandins PGA1 and 15‐deoxy‐Δ12,14‐PGJ2: Role of glutathione

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Hypothemycin, a fungal natural product, identifies therapeutic targets in Trypanosoma brucei

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Reactivity assessment of chalcones by a kinetic thiol assay

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A Fluorescence-Based Thiol Quantification Assay for Ultra-High-Throughput Screening for Inhibitors of Coenzyme A Production

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Melampomagnolide B: A new antileukemic sesquiterpene

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Kinetic Template‐Guided Tethering of Fragments

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Application of structure–activity relationships to investigate the molecular mechanisms of hepatocyte toxicity and electrophilic reactivity of α,β‐unsaturated aldehydes

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Covalent modification of the active site of carbamyl phosphate synthetase by 5'-p-fluorosulfonylbenzoyladenosine. Direct evidence for two functionally different ATP-binding sites.

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NADPH Alkenal/One Oxidoreductase Activity Determines Sensitivity of Cancer Cells to the Chemotherapeutic Alkylating Agent Irofulven

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Characterization of Irreversible Kinase Inhibitors by Directly Detecting Covalent Bond Formation: A Tool for Dissecting Kinase Drug Resistance

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Opening or Closing the Lock? When Reactivity Is the Key to Biological Activity

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Anti-selective Michael addition of thiols and their analogs to nitro olefins

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A novel Bruton’s tyrosine kinase inhibitor CC-292 in combination with the proteasome inhibitor carfilzomib impacts the bone microenvironment in a multiple myeloma model with resultant antimyeloma activity

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Synthesis and biological properties of new α-methylene-γ-butyrolactones and α,β-unsaturated δ-lactones

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Anti-inflammatory effect of lucidone in mice via inhibition of NF-κB/MAP kinase pathway

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Activity-based proteomics: enzyme chemistry redux

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Large‐Scale Synthesis of New Pyranoid Building Blocks Based on Aldolase‐Catalysed Carbon‐Carbon Bond Formation

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Cyclopentenediones, inhibitors of farnesyl protein transferase and anti-tumor compounds, isolated from the fruit of Lindera erythrocarpa Makino

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COVALENT DRUGS FORM LONG-LIVED TIES

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The reaction of PGA1 with sulfhydryl groups; a component in the binding of A-type prostaglandins to proteins

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Antibacterial Activity and Chemical Structure of Diterpenoids

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Cyclopentenone Prostaglandins with Dienone Structure Promote Cross-Linking of the Chemoresistance-Inducing Enzyme Glutathione Transferase P1-1

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Mechanistic Study of the Reaction of Thiol‐Containing Enzymes with α,β‐Unsaturated Carbonyl Substrates by Computation and Chemoassays

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Diterpenoids of Rabdosia Species

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Direct evidence for the covalent modification of glutathione-S-transferase P1-1 by electrophilic prostaglandins: Implications for enzyme inactivation and cell survival

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2,5-Disubstituted 3,4-dihydro-2H-benzo[b][1,4]thiazepines as potent and selective V2 arginine vasopressin receptor antagonists

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Lucidone Inhibits iNOS and COX-2 Expression in LPS-Induced RAW 264.7 Murine Macrophage Cells via NF-κB and MAPKs Signaling Pathways

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Pyrrocidine A, a metabolite of endophytic fungi, has a potent apoptosis-inducing activity against HL60 cells through caspase activation via the Michael addition

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Synthesis and angiotensin-converting enzyme inhibitory activity of 3-(mercaptomethyl)-2-oxo-1-pyrrolidineacetic acids and 3-(mercaptomethyl)-2-oxo-1-piperidineacetic acids

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Proteomic studies on protein modification by cyclopentenone prostaglandins: Expanding our view on electrophile actions

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Studies on structurally simple α,β-butenolides. III.

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The C-Terminus of H-Ras as a Target for the Covalent Binding of Reactive Compounds Modulating Ras-Dependent Pathways

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Reactions of some cyclopentenones with selected cysteine derivatives and biological activities of the product thioethers

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The reaction of some nuclear substituted acyclic conjugated styryl ketones and related Mannich bases with ethanethiol

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Covalent Reactions of Wortmannin under Physiological Conditions

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Redox Regulation of Protein Tyrosine Phosphatases

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Chiral 1,4-diazepinones and 1,4-thiazepinones by diastereoselective ring chain transformation of α,β unsaturated lactones or lactams

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Fukui Function

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Susceptibility of the Antioxidant Selenoenyzmes Thioredoxin Reductase and Glutathione Peroxidase to Alkylation-Mediated Inhibition by Anticancer Acylfulvenes

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Substituent Effects on the Reactivity of Benzoquinone Derivatives with Thiols

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Protein alkylation by the α,β‐unsaturated aldehyde acrolein. A reversible mechanism of electrophile signaling?

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Novel Bruton's tyrosine kinase inhibitors currently in development

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Reactions of Formylchromone Derivatives; 31. A Facile Synthesis of Fused Benzopyrano-benzothiazepinones, -benzoxazepinones, and -benzodiazepinones

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Total synthesis of human chymase inhibitor methyllinderone and structure–activity relationships of its derivatives

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Synthesis and Biological Evaluation of Antitumor‐Active Arglabin Derivatives

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A Highly Selective Fluorescent Probe for Detection of Biological Samples Thiol and Its Application in Living Cells

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Probing the Selectivity and Protein⋅Protein Interactions of a Nonreducing Fungal Polyketide Synthase Using Mechanism-Based Crosslinkers

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Reactivity of α,β-unsaturated carbonyl compounds towards nucleophilic addition reaction: a local hard–soft acid–base approach

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Benzylidene cyclopentenediones: First irreversible inhibitors against botulinum neurotoxin A’s zinc endopeptidase

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Reaction of antitumor hydroxymethylacylfulvene (HMAF) with thiols

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A Competitive Fluorescence Assay to Measure the Reactivity of Compounds

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Reactions of formylchromone derivatives. Part 2. Addition reactions of 3-(aryliminomethyl)chromones

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α-Methylene-γ-butyrolactones attenuate Staphylococcus aureus virulence by inhibition of transcriptional regulation

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Understanding the Structural Requirements for Activators of the Kef Bacterial Potassium Efflux System

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Rational Design of Resorcylic Acid Lactone Analogues as Covalent MNK1/2 Kinase Inhibitors by Tuning the Reactivity of an Enamide Michael Acceptor

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New α-methylene-γ-butyrolactones with antimycobacterial properties

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Rates and Equilibria of the Michael-Type Addition of Benzenethiol to 2-Cyclopenten-1-ones

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Protein Reactivity of Natural Product-Derived γ-Butyrolactones

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Synthesis and antileukemic activities of C1–C10-modified parthenolide analogues

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New insights into the water-solubilization of thiol-sensitive fluorogenic probes based on long-wavelength 7-hydroxycoumarin scaffolds

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Fluorescence turn-on probe for biothiols: intramolecular hydrogen bonding effect on the Michael reaction

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Molecular Editing of Kinase‐Targeting Resorcylic Acid Lactones (RAL): Fluoroenone RAL

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Synthesis and biological properties of macrolactam analogs of the natural product macrolide (−)-A26771B

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Ratiometric fluorescence probes based on a Michael acceptor type of coumarin and their application for the multichannel imaging of in vivo glutathione

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The Thia‐Michael Reactivity of Zerumbone and Related Cross‐Conjugated Dienones: Disentangling Stoichiometry, Regiochemistry, and Addition Mode with an NMR‐Spectroscopy‐Based Cysteamine Assay

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Highly selective fluorescence turn-on probe for glutathione

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Convenient two-step stereospecific hydroxy-substitution with retention in β-hydroxy-δ-lactones. 4 ()-heterosubstituted mevinolin and -analogs

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Fluoride ion-catalyzed conjugate addition for easy synthesis of 3-sulfanylpropionic acid from thiol and α,β-unsaturated carboxylic acid

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Synthetic studies on the esperamicin/calicheamicin antitumor antibiotics. Conjugate addition of thiol to initiate 1,4-diyl formation

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11,13-dihydro-dehydroleucodine, a derivative of dehydroleucodine with an inactivated alkylating function conserves the anti-proliferative activity in G2 but does not cause cytotoxicity

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Profiling patterns of glutathione reductase inhibition by the natural product illudin S and its acylfulvene analogues

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Design, synthesis and biological evaluation of FLT3 covalent inhibitors with a resorcylic acid core

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Mechanism of Action of Thalassospiramides, A New Class of Calpain Inhibitors

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