ArticleChemMedChem2015
Synthetic and Biological Studies of Sesquiterpene Polygodial: Activity of 9-Epipolygodial against Drug-Resistant Cancer Cells.
Article in ChemMedChem, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
What it found
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Who cites it
11 citing papers in PubMed, 23 citations in OpenAlex.
- Semisynthetic Derivatives of Polygodial as α-Glucosidase and α-Amylase Inhibitors: In Vitro Evaluation, Molecular Docking and Molecular Dynamics Simulation.Pharmaceutics · 2026Article
- Article
- Anticancer Activity of Natural and Semi-Synthetic Drimane and Coloratane Sesquiterpenoids.Molecules (Basel, Switzerland) · 2022Review
- Stimulation of ROS Generation by Extract ofAntioxidants (Basel, Switzerland) · 2021Article
- Inhibition of Growth of Colon Tumors and Proliferation of HT-29 Cells byOxidative medicine and cellular longevity · 2021Article
- Semi-synthetic cinnamodial analogues: Structural insights into the insecticidal and antifeedant activities of drimane sesquiterpenes against the mosquito Aedes aegypti.PLoS neglected tropical diseases · 2020Article
- Novel polygodial analogs P3 and P27: Efficacious therapeutic agents disrupting mitochondrial function in oral squamous cell carcinoma.International journal of oncology · 2018Article
- Polygodial analog induces apoptosis in LNCaP prostate cancer cells.European journal of pharmacology · 2018Article
- Investigation of the electrophilic reactivity of the biologically active marine sesquiterpenoid onchidal and model compounds.Beilstein journal of organic chemistry · 2018Article
- Covalent modification of biological targets with natural products through Paal-Knorr pyrrole formation.Natural product reports · 2017Review
- Wittig derivatization of sesquiterpenoid polygodial leads to cytostatic agents with activity against drug resistant cancer cells and capable of pyrrolylation of primary amines.European journal of medicinal chemistry · 2015Article
Corrections and comments
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Authors and funding
24 authors at 10 institutions in 6 countries.
Funding
Abstract
Polygodial, a terpenoid dialdehyde isolated from Polygonum hydropiper L., is a known agonist of the transient receptor potential vanilloid 1 (TRPV1). In this investigation a series of polygodial analogues were prepared and investigated for TRPV1-agonist and anticancer activities. These experiments led to the identification of 9-epipolygodial, which has antiproliferative potency significantly exceeding that of polygodial. 9-Epipolygodial was found to maintain potency against apoptosis-resistant cancer cells as well as those displaying the multidrug-resistant (MDR) phenotype. In addition, the chemical feasibility for the previously proposed mechanism of action of polygodial, involving the formation of a Paal-Knorr pyrrole with a lysine residue on the target protein, was demonstrated by the synthesis of a stable polygodial pyrrole derivative. These studies reveal rich chemical and biological properties associated with polygodial and its direct derivatives. These compounds should inspire further work in this area aimed at the development of new pharmacological agents, or the exploration of novel mechanisms of covalent modification of biological molecules with natural products.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.