Chalcone and its analogs: Therapeutic and diagnostic applications in Alzheimer’s disease

Pritam Thapa; Sunil P. Upadhyay; William Z. Suo; Vikas Singh; Prajwal Gurung; Eung Seok Lee; Ram Sharma; Mukut Sharma

doi:10.1016/j.bioorg.2021.104681

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Chalcone and its analogs: Therapeutic and diagnostic applications in Alzheimer’s disease

Journal article

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Peer reviewed

Chalcone and its analogs: Therapeutic and diagnostic applications in Alzheimer’s disease

Pritam Thapa, Sunil P. Upadhyay, William Z. Suo, Vikas Singh, Prajwal Gurung, Eung Seok Lee, Ram Sharma and Mukut Sharma

Bioorganic chemistry, Vol.108, pp.104681-104681

03/2021

DOI: 10.1016/j.bioorg.2021.104681

PMCID: PMC7928223

PMID: 33571811

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https://www.ncbi.nlm.nih.gov/pmc/articles/7928223View

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Abstract

[Display omitted] Chalcone [(E)-1,3-diphenyl-2-propene-1-one], a small molecule with α, β unsaturated carbonyl group is a precursor or component of many natural flavonoids and isoflavonoids. It is one of the privileged structures in medicinal chemistry. It possesses a wide range of biological activities encouraging many medicinal chemists to study this scaffold for its usefulness to oncology, infectious diseases, virology and neurodegenerative diseases including Alzheimer’s disease (AD). Small molecular size, convenient and cost-effective synthesis, and flexibility for modifications to modulate lipophilicity suitable for blood brain barrier (BBB) permeability make chalcones a preferred candidate for their therapeutic and diagnostic potential in AD. This review summarizes and highlights the importance of chalcone and its analogs as single target small therapeutic agents, multi-target directed ligands (MTDLs) as well as molecular imaging agents for AD. The information summarized here will guide many medicinal chemist and researchers involved in drug discovery to consider chalcone as a potential scaffold for the development of anti-AD agents including theranostics.

Alzheimer’s disease

Amyloid beta inhibition

Chalcone

Cholinesterase inhibitors

Molecular probes

Multi-target directed ligands

Neuroinflammation

Theranostic

Details

Title: Subtitle: Chalcone and its analogs: Therapeutic and diagnostic applications in Alzheimer’s disease
Creators: Pritam Thapa - Drug Discovery Program, Midwest Veterans' Biomedical Research Foundation, KCVA Medical Center, Kansas City, MO 64128, USA.
Sunil P. Upadhyay - Drug Discovery Program, Midwest Veterans' Biomedical Research Foundation, KCVA Medical Center, Kansas City, MO 64128, USA.
William Z. Suo - Veterans Health Administration
Vikas Singh - Kansas City VA Medical Center
Prajwal Gurung - University of Iowa
Eung Seok Lee - Yeungnam University
Ram Sharma - Drug Discovery Program, Midwest Veterans' Biomedical Research Foundation, KCVA Medical Center, Kansas City, MO 64128, USA.
Mukut Sharma - Drug Discovery Program, Midwest Veterans' Biomedical Research Foundation, KCVA Medical Center, Kansas City, MO 64128, USA.
Resource Type: Journal article
Publication Details: Bioorganic chemistry, Vol.108, pp.104681-104681
DOI: 10.1016/j.bioorg.2021.104681
PMID: 33571811
PMCID: PMC7928223
NLM abbreviation: Bioorg Chem
ISSN: 0045-2068
eISSN: 1090-2120
Publisher: Elsevier Inc
Grant note: DOI: 10.13039/100000002, name: National Institutes of Health
Language: English
Date published: 03/2021
Academic Unit: Infectious Diseases; Internal Medicine
Record Identifier: 9984359883002771

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