Synthesis of Rocaglamide Hydroxamates and Related Compounds as Eukaryotic Translation Inhibitors: Synthetic and Biological Studies

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Enantioselective Synthesis of the Complex Rocaglate (−)‐Silvestrol

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Total Synthesis of the Potent Anticancer Aglaia Metabolites (−)-Silvestrol and (−)-Episilvestrol and the Active Analogue (−)-4′-Desmethoxyepisilvestrol

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Biomimetic Photocycloaddition of 3‐Hydroxyflavones: Synthesis and Evaluation of Rocaglate Derivatives as Inhibitors of Eukaryotic Translation

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Total synthesis of (±)-rocaglamide and some aryl analogues

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Silvestrol regulates G2/M checkpoint genes independent of p53 activity.

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Novel Flavaglines Displaying Improved Cytotoxicity

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General Reactivity of 2-Lithiobenzothiazole to Various Electrophiles and the Use as a Formyl Anion Equivalent in the Synthesis of α-Hydroxy Carbonyl Compounds

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Targeting Translation Dependence in Cancer

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Design and synthesis of potent Gram-negative specific LpxC inhibitors

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Beyond the MEK-pocket: Can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK?

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Design, synthesis, and biological evaluation of simplified α-Keto heterocycle, trifluoromethyl ketone, and formyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase

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Design and Evaluation of Hydroxamate Derivatives as Metal-Mediated Inhibitors of a Protein Tyrosine Kinase

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RNA G-quadruplexes cause eIF4A-dependent oncogene translation in cancer

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Sensitization of renal carcinoma cells to TRAIL-induced apoptosis by rocaglamide and analogs

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Tight Coordination of Protein Translation and HSF1 Activation Supports the Anabolic Malignant State

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Chemical probes and drug leads from advances in synthetic planning and methodology

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Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase

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Rocaglamide, silvestrol and structurally related bioactive compounds from Aglaia species

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Targeting MYC in multiple myeloma

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Evidence for a Functionally Relevant Rocaglamide Binding Site on the eIF4A–RNA Complex

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Targeting Translation Initiation Bypasses Signaling Crosstalk Mechanisms That Maintain High MYC Levels in Colorectal Cancer

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eIF4A supports an oncogenic translation program in pancreatic ductal adenocarcinoma

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CRISPR-Mediated Drug-Target Validation Reveals Selective Pharmacological Inhibition of the RNA Helicase, eIF4A

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Transcription and Translation Inhibitors in Cancer Treatment

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Synthetic Silvestrol Analogues as Potent and Selective Protein Synthesis Inhibitors

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Flavaglines as Potent Anticancer and Cytoprotective Agents

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Targeting the eIF4A RNA helicase as an anti-neoplastic approach

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Flavaglines: Potent Anticancer Drugs that Target Prohibitins and the Helicase eIF4A

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Amidino-Rocaglates: A Potent Class of eIF4A Inhibitors

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Rocaglates Induce Gain-of-Function Alterations to eIF4A and eIF4F

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Inhibiting the oncogenic translation program is an effective therapeutic strategy in multiple myeloma

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Hydroxamate, a Key Pharmacophore Exhibiting a Wide Range of Biological Activities

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A Novel Class of Small Molecule Compounds that Inhibit Hepatitis C Virus Infection by Targeting the Prohibitin-CRaf Pathway

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Two Unusual Polycyclic Polyprenylated Acylphloroglucinols, Including a Pair of Enantiomers from Garcinia multiflora

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Synthesis of Biotinylated Episilvestrol: Highly Selective Targeting of the Translation Factors eIF4AI/II

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Enantioselective Photocycloaddition of 3-Hydroxyflavones: Total Syntheses and Absolute Configuration Assignments of (+)-Ponapensin and (+)-Elliptifoline

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Highly selective fluorimetric sensor for Cu 2+ and Hg 2+ using a benzothiazole-based receptor in semi-aqueous media and molecular docking studies

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The integrated stress response mediates necrosis in murine Mycobacterium tuberculosis granulomas

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Synthesis of Each Enantiomer of Rocaglamide by Means of a Palladium(0)‐Catalyzed Nazarov‐Type Cyclization

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Targeting the eIF4A RNA helicase blocks translation of the MUC1-C oncoprotein

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Functional mimicry revealed by the crystal structure of an eIF4A:RNA complex bound to the interfacial inhibitor, desmethyl pateamine A

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eIF4A Inhibitors Suppress Cell-Cycle Feedback Response and Acquired Resistance to CDK4/6 Inhibition in Cancer

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Remodeling Natural Products: Chemistry and Serine Hydrolase Activity of a Rocaglate-Derived β-Lactone

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Synthesis of Aza‐Rocaglates via ESIPT‐Mediated (3+2) Photocycloaddition

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Targeting eIF4A-Dependent Translation of KRAS Signaling Molecules

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Targeting the DEAD-Box RNA Helicase eIF4A with Rocaglates—A Pan-Antiviral Strategy for Minimizing the Impact of Future RNA Virus Pandemics

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Recent Advances in the Synthesis of Flavaglines, a Family of Potent Bioactive Natural Compounds Originating from Traditional Chinese Medicine

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Cytostatic and Cytotoxic Natural Products against Cancer Cell Models

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KDM5A Regulates a Translational Program that Controls p53 Protein Expression

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Chemical Synthesis Enables Structural Reengineering of Aglaroxin C Leading to Inhibition Bias for Hepatitis C Viral Infection

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Rocaglates as dual-targeting agents for experimental cerebral malaria

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Targeting translation initiation by synthetic rocaglates for treating MYC-driven lymphomas

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EIF4A inhibition targets bioenergetic homeostasis in AML MOLM-14 cells in vitro and in vivo and synergizes with cytarabine and venetoclax

Fooks, K., Galicia-Vázquez, G., Gife, V., Schcolnik-Cabrera, A., Nouhi, Z., Poon, W. W. L., Luo, V. M., Rys, R., Aloyz, R., Orthwein, A., et al. (2022) · Journal of experimental & clinical cancer research : CR · doi:10.1186/s13046-022-02542-8 · Cited by 23 · see citing works

Intercepted Retro-Nazarov Reaction: Syntheses of Amidino-Rocaglate Derivatives and Their Biological Evaluation as eIF4A Inhibitors

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The rocaglate CR-31-B (−) inhibits SARS-CoV-2 replication at non-cytotoxic, low nanomolar concentrations in vitro and ex vivo

Müller, C., Obermann, W., Karl, N., Wendel, H., Taroncher‐Oldenburg, G., Pleschka, S., Hartmann, R. K., Grünweller, A., & Ziebuhr, J. (2021) · Antiviral Research · doi:10.1016/j.antiviral.2021.105012 · Cited by 33 · see citing works

Comparative phytochemistry of flavaglines (= rocaglamides), a group of highly bioactive flavolignans from Aglaia species (Meliaceae)

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A photochemical flow reactor for large scale syntheses of aglain and rocaglate natural product analogues

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NRF2 Activation Confers Resistance to eIF4A Inhibitors in Cancer Therapy

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Channeling macrophage polarization by rocaglates increases macrophage resistance to Mycobacterium tuberculosis

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A second-generation eIF4A RNA helicase inhibitor exploits translational reprogramming as a vulnerability in triple-negative breast cancer

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Drug-induced Stress Granule Formation Protects Sensory Hair Cells in Mouse Cochlear Explants During Ototoxicity

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Translation Inhibition by Rocaglates Is Independent of eIF4E Phosphorylation Status

Chu, J., Cencic, R., Wang, W., Porco, J. A. J., & Pelletier, J. (2015) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-15-0409 · Cited by 25 · see citing works

Solvent-controlled difluoromethylation of 2′-hydroxychalcones for divergent synthesis of 2′-difluoromethoxychalcones and 2,2-difluoro-3-styryl-2,3-dihydrobenzofuran-3-ols

Hua, M., Wang, W., Liu, W.-H., Wang, T., Zhang, Q., Huang, Y., & Zhu, W. (2015) · Journal of Fluorine Chemistry · doi:10.1016/j.jfluchem.2015.11.003 · Cited by 25 · see citing works

Simplified Silvestrol Analogues with Potent Cytotoxic Activity

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Assessing eukaryotic initiation factor 4F subunit essentiality by CRISPR-induced gene ablation in the mouse

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Rocaglates as Antivirals: Comparing the Effects on Viral Resistance, Anti-Coronaviral Activity, RNA-Clamping on eIF4A and Immune Cell Toxicity

Obermann, W., Friedrich, A., Madhugiri, R., Klemm, P., Mengel, J. P., Hain, T., Pleschka, S., Wendel, H., Hartmann, R. K., Schiffmann, S., et al. (2022) · Viruses · doi:10.3390/v14030519 · Cited by 19 · see citing works

Update on Phytochemical and Biological Studies on Rocaglate Derivatives from Aglaia Species

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Halogenated Rocaglate Derivatives: Pan-antiviral Agents against Hepatitis E Virus and Emerging Viruses

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Eukaryotic Translation Initiation Factor 4AI: A Potential Novel Target in Neuroblastoma

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eIF4A controls translation of estrogen receptor alpha and is a therapeutic target in advanced breast cancer

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Throwing a monkey wrench in the motor: Targeting DExH/D box proteins with small molecule inhibitors

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Identification of structurally re-engineered rocaglates as inhibitors against hepatitis E virus replication

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Mouse Models of c-myc Deregulation Driven by IgH Locus Enhancers as Models of B-Cell Lymphomagenesis

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Protein–RNA interactions mediated by silvestrol—insight into a unique molecular clamp

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Synthesis of Each Enantiomer of Rocaglamide by Means of a Palladium(0)‐Catalyzed Nazarov‐Type Cyclization

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Strategic Diastereoselective C1 Functionalization in the Aza-Rocaglamide Scaffold toward Natural Product-Inspired eIF4A Inhibitors

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Exploring the targeting spectrum of rocaglates among eIF4A homologs

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Discovery of an eIF4A Inhibitor with a Novel Mechanism of Action

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Phase Transfer Catalysis Extends The Scope of The Algar–Flynn–Oyamada Synthesis of 3-Hydroxyflavones

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Suppression of eukaryotic initiation factor 4E prevents chemotherapy-induced alopecia

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Oxo-aglaiastatin-Mediated Inhibition of Translation Initiation

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Tracing MYC Expression for Small Molecule Discovery

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Targeted inhibition of mRNA translation initiation factors as a novel therapeutic strategy for mature B-cell neoplasms

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Targeting eIF4A using rocaglate CR‑1‑31B sensitizes gallbladder cancer cells to TRAIL‑mediated apoptosis through the translational downregulation of c‑FLIP

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Comparing the Effects of Rocaglates on Energy Metabolism and Immune Modulation on Cells of the Human Immune System

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Total synthesis of a biotinylated rocaglate: Selective targeting of the translation factors eIF4AI/II

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How to nurture natural products to create new therapeutics: Strategic innovations and molecule-to-medicinal insights into therapeutic advancements

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Identification of Rocaglate Acyl Sulfamides as Selective Inhibitors of Glioblastoma Stem Cells

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A forward genetic screen identifies modifiers of rocaglate responsiveness

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Programmable modulation of ribosomal frameshifting by mRNA targeting CRISPR-Cas12a system

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Discovery of RNA-Protein Molecular Clamps Using Proteome-Wide Stability Assays

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Amidino-rocaglates (ADRs), a class of synthetic rocaglates, are potent inhibitors of SARS-CoV-2 replication through inhibition of viral protein synthesis

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1-Aminomethyl SAR in a novel series of flavagline-inspired eIF4A inhibitors: Effects of amine substitution on cell potency and in vitro PK properties

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Bioactive Flavaglines: Synthesis and Pharmacology

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Synthesis of cis-Oriented Vicinal Diphenylethylenes through a Lewis Acid-Promoted Annulation of Oxotriphenylhexanoates

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Design and Synthesis of Cytotoxic Water-Soluble Rocaglaol Derivatives against HEL Cells by Inhibiting Fli-1

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In Vitro Discovery of a Therapeutic Lead for HFMD From a Library Screen of Rocaglates/Aglains

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Activity of Didesmethylrocaglamide in High Grade Serous Ovarian Cancer Using Preclinical In Vitro and In Vivo Models

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Targeting eIF4A-dependent translation in genetically complex sarcoma

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Current and Emerging Therapies Targeting Translation

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A Phase I Pharmacologic Study of Necitumumab (IMC-11F8), a Fully Human IgG1 Monoclonal Antibody

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Understanding the role of stress granules in the inner ear

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Channeling macrophage polarization via selective translation inhibition by rocaglates increases macrophage resistance to Mycobacterium tuberculosisPreprint

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EIF4A inhibition targets bioenergetic homeostasis in AML and synergizes with cytarabine and venetoclaxPreprint

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Data from Targeting eIF4A-Dependent Translation of KRAS Signaling Molecules

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Data from Targeting eIF4A-Dependent Translation of KRAS Signaling Molecules

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Structural and biochemical studies of virus : host interactions in HIV-1

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Assessment of Rocaglates and Targeted Derivatives as Selective Inhibitors of Glioblastoma Stem CellsPreprint

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Additional file 1 of EIF4A inhibition targets bioenergetic homeostasis in AML MOLM-14 cells in vitro and in vivo and synergizes with cytarabine and venetoclax

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Development of new approaches for the synthesis of flavaglines

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Flavaglines as cross-kingdom translation inhibitors: Heavy halides at C6 potentiate antineoplastic, antiviral, and antifungal activities

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Performing the Syntheses of Rocaglamide Analogs

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Progress toward a computationally-directed synthesis of rocaglamide analogs for cancer treatment

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Biomimetic Photocycloaddition of 3‐Hydroxyflavones: Synthesis and Evaluation of Rocaglate Derivatives as Inhibitors of Eukaryotic Translation

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楝酰胺(rocaglamide)全合成研究进展

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Synthetic Silvestrol Analogues as Potent and Selective Protein Synthesis Inhibitors

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