ArticleBioorganic & medicinal chemistry2009
The marine natural-derived inhibitors of glycogen synthase kinase-3beta phenylmethylene hydantoins: In vitro and in vivo activities and pharmacophore modeling.
Article in Bioorganic & medicinal chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 52 citations in OpenAlex.
- Recent Development in Hydantoins, Thiohydantoins, and Selenohydantoins as Anticancer Agents: Structure-activity Relationship and Design Strategies.Mini reviews in medicinal chemistry · 2025Review
- Synthesis and Evaluation of 5-(Heteroarylmethylene)hydantoins as Glycogen Synthase Kinase-3β Inhibitors.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Natural Bioactive Compounds from Marine Invertebrates That Modulate Key Targets Implicated in the Onset of Type 2 Diabetes Mellitus (T2DM) and Its Complications.Pharmaceutics · 2023Review
- Marine Natural Products with Activities against Prostate Cancer: Recent Discoveries.International journal of molecular sciences · 2023Review
- Review
- Bioactive natural products from marine sponges belonging to family Hymedesmiidae.RSC advances · 2021Review
- Investigation of naphthofuran moiety as potential dual inhibitor against BACE-1 and GSK-3β: molecular dynamics simulations, binding energy, and network analysis to identify first-in-class dual inhibitors against Alzheimer's disease.Journal of molecular modeling · 2017Article
- Marine Organisms with Anti-Diabetes Properties.Marine drugs · 2016Review
- Article
- Glycogen synthase kinase 3β orchestrates microtubule remodeling in compensatory glomerular adaptation to podocyte depletion.The Journal of biological chemistry · 2015Article
- Bioactive marine drugs and marine biomaterials for brain diseases.Marine drugs · 2014Article
- Small-Molecule Inhibitors of GSK-3: Structural Insights and Their Application to Alzheimer's Disease Models.International journal of Alzheimer's disease · 2012Article
- Manzamine A as a novel inhibitor of herpes simplex virus type-1 replication in cultured corneal cells.Planta medica · 2011Article
- Marine bioactives as functional food ingredients: potential to reduce the incidence of chronic diseases.Marine drugs · 2011Review
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
The Red Sea sponge Hemimycale arabica afforded the known (Z)-5-(4-hydroxybenzylidene)-hydantoin (1). This natural phenylmethylene hydantoin (PMH) 1 and the synthetic (Z)-5-(4-(ethylthio)benzylidene)-hydantoin (2) showed potent in vitro and in vivo anti-growth and anti-invasive properties against PC-3M prostate cancer cells in MTT, spheroid disaggregation, and in mice models. To explore a possible molecular target of PMHs, the most potent synthetic analogue 2 has been virtually screened against various protein kinases. Molecular modeling study has shown that 2 can be successfully docked within the binding pocket of glycogen synthase kinase-3beta (GSK-3beta) similar to the well-known GSK-3beta inhibitor I-5. Several PMHs showed potent in vitro GSK-3beta inhibitory activity with an IC(50) range of 4-20microM. The most potent analogue 3 showed a significant increase in liver glycogen level at the 5, 15, and 25mg/kg dose levels, in vivo. Pharmacophore model was built and validated using in-house database of active and inactive GSK-3beta inhibitors. The GSK-3beta inhibitory activity of PMHs entitles them to be potential leads for the treatment of cancer, Alzheimer's disease, bipolar disorders, stroke, different tau pathologies, and type-2 diabetes.
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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.