ArticleBioorganic & medicinal chemistry2015
Bivalent ligands incorporating curcumin and diosgenin as multifunctional compounds against Alzheimer's disease.
Article in Bioorganic & medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed.
- Neuroprotective Effects of Sorghum Polyphenol in Alzheimer's Disease: In Vitro and In Silico Analyses.Nutrients · 2026Article
- Diosgenin derivative ML5 attenuates MPTP-induced neuronal impairment via regulating AMPK/PGC-1α-mediated mitochondrial biogenesis and fusion/fission.American journal of translational research · 2024Article
- Diosgenin: An Updated Pharmacological Review and Therapeutic Perspectives.Oxidative medicine and cellular longevity · 2022Review
- Curcumin, Resveratrol and Cannabidiol as Natural Key Prototypes in Drug Design for Neuroprotective Agents.Current neuropharmacology · 2022Review
- Synthesis of Anti-Inflammatory Spirostene-Pyrazole Conjugates by a Consecutive Multicomponent Reaction of Diosgenin with Oxalyl Chloride, Arylalkynes and Hydrazines or Hydrazones.Molecules (Basel, Switzerland) · 2021Article
- A comparison of the location in membranes of curcumin and curcumin-derived bivalent compounds with potential neuroprotective capacity for Alzheimer's disease.Colloids and surfaces. B, Biointerfaces · 2021Article
- Curcumin as Scaffold for Drug Discovery against Neurodegenerative Diseases.Biomedicines · 2021Review
- Synthesis and Pharmacological Effects of Diosgenin-Betulinic Acid Conjugates.Molecules (Basel, Switzerland) · 2020Article
- Therapeutic Potential of Diosgenin and Its Major Derivatives against Neurological Diseases: Recent Advances.Oxidative medicine and cellular longevity · 2020Review
- Development of bivalent compounds as potential neuroprotectants for Alzheimer's disease.Bioorganic & medicinal chemistry letters · 2019Article
- Synthesis and potent cytotoxic activity of a novel diosgenin derivative and its phytosomes against lung cancer cells.Beilstein journal of nanotechnology · 2019Article
- Design and characterization of bivalent compounds as potential neuroprotectants for Alzheimer's disease: Impact of the spacer on biological activity.Bioorganic & medicinal chemistry letters · 2018Article
- Insights into the Impact of a Membrane-Anchoring Moiety on the Biological Activities of Bivalent Compounds As Potential Neuroprotectants for Alzheimer's Disease.Journal of medicinal chemistry · 2018Article
- Chronic diseases, inflammation, and spices: how are they linked?Journal of translational medicine · 2018Review
- The Anti-Amyloid-β and Neuroprotective Properties of a Novel Tricyclic Pyrone Molecule.Journal of Alzheimer's disease : JAD · 2017Article
- Development and Structural Modification of BACE1 Inhibitors.Molecules (Basel, Switzerland) · 2016Review
- Mechanistic Insight of Bivalent Compound 21MO as Potential Neuroprotectant for Alzheimer's Disease.Molecules (Basel, Switzerland) · 2016Article
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4 authors.
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Abstract
In an effort to combat the multifaceted nature of Alzheimer's disease (AD) progression, a series of multifunctional, bivalent compounds containing curcumin and diosgenin were designed, synthesized, and biologically characterized. Screening results in MC65 neuroblastoma cells established that compound 38 with a spacer length of 17 atoms exhibited the highest protective potency with an EC50 of 111.7 ± 9.0 nM. A reduction in protective activity was observed as spacer length was increased up to 28 atoms and there is a clear structural preference for attachment to the methylene carbon between the two carbonyl moieties of curcumin. Further study suggested that antioxidative ability and inhibitory effects on amyloid-β oligomer (AβO) formation may contribute to the neuroprotective outcomes. Additionally, compound 38 was found to bind directly to Aβ, similar to curcumin, but did not form complexes with the common biometals Cu, Fe, and Zn. Altogether, these results give strong evidence to support the bivalent design strategy in developing novel compounds with multifunctional ability for the treatment of AD.
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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.