The DOI matches its Crossref record; 10 of the 10 references it cites were found in a registry or an index.
Design, Synthesis, and Evaluation of Multitarget-Directed Resveratrol Derivatives for the Treatment of Alzheimer’s Disease
Open accessAbstract
A series of multitarget-directed resveratrol derivatives was designed and synthesized for the treatment of Alzheimer's disease (AD). In vitro studies indicated that most of the target compounds exhibit significant inhibition of self-induced β-amyloid (Aβ) aggregation and Cu(II)-induced Aβ1-42 aggregation and acted as potential antioxidants and biometal chelators. In particular, compounds 5d and 10d are potential lead compounds for AD therapy (5d, IC50 = 7.56 μM and 10d, IC50 = 6.51 μM for self-induced Aβ aggregation; the oxygen radical absorbance capacity assay using fluorescein (ORAC-FL) values are 4.72 and 4.70, respectively). Moreover, these compounds are capable of disassembling the highly structured Aβ fibrils generated by self- and Cu(II)-induced Aβ aggregation. Furthermore, 5d crossed the blood-brain barrier (BBB) in vitro and did not exhibit any acute toxicity in mice at doses of up to 2000 mg/kg. Taken together, the data indicate that 5d is a very promising lead compound for AD.
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Cites
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Resveratrol and health—A comprehensive review of human clinical trials
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Different Mechanisms of Oxidative Stress and Neurotoxicity for Alzheimer‘s Aβ(1−42) and Aβ(25−35)
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Cholinesterase Inhibitors and Beyond
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Small Molecule Modulators of Copper-Induced Aβ Aggregation
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Bifunctional Compounds for Controlling Metal-Mediated Aggregation of the Aβ42Peptide
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Chromone as a Privileged Scaffold in Drug Discovery: Recent Advances: Miniperspective
Reis, J., Gaspar, A., Milhazes, N., & Borges, F. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b01720 · Cited by 414
Neuroprotective Mechanisms of Resveratrol in Alzheimer’s Disease: Role of SIRT1
Gomes, B. A. Q., Silva, J. P. B., Romeiro, C. F. R., dos Santos, S. M., Rodrigues, C. A., Gonçalves, P. R., Sakai, J. T., Mendes, P. F. S., Varela, E. L. P., & Monteiro, M. C. (2018) · Oxidative Medicine and Cellular Longevity · doi:10.1155/2018/8152373 · Cited by 403
Guzior, N., Wi.eckowska, A., Panek, D., & Malawska, B. (2014) · Current Medicinal Chemistry · doi:10.2174/0929867321666141106122628 · Cited by 323
Resveratrol: A miraculous natural compound for diseases treatment
Koushki, M., Amiri‐Dashatan, N., Ahmadi, N., Abbaszadeh, H., & Rezaei‐Tavirani, M. (2018) · Food Science & Nutrition · doi:10.1002/fsn3.855 · Cited by 316
Metadata
- Authors
- Lu, C., Guo, Y., Yan, J., Luo, Z., Luo, H.-B., Yan, M., Huang, L., & Li, X.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2013-07-08
- Volume
- 56
- Issue
- 14
- Pages
- 5843-5859
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W1975792122
- Cited by
- 226
- References
- 10
- FWCI
- 13.47
- Type
- journal article
- Language
- en
- Open access
- green
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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