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Chalcone and its analogs: Therapeutic and diagnostic applications in Alzheimer’s disease
[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 activi...
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| Published in: | Bioorganic chemistry 2021-03, Vol.108, p.104681-104681, Article 104681 |
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| Main Authors: | , , , , , , , |
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| cited_by | cdi_FETCH-LOGICAL-c529t-5218eaec654377dc04436ec5b756ea7ef3112ebcf901c069b37221dbc540492c3 |
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| cites | cdi_FETCH-LOGICAL-c529t-5218eaec654377dc04436ec5b756ea7ef3112ebcf901c069b37221dbc540492c3 |
| container_end_page | 104681 |
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| container_start_page | 104681 |
| container_title | Bioorganic chemistry |
| container_volume | 108 |
| creator | Thapa, Pritam Upadhyay, Sunil P. Suo, William Z. Singh, Vikas Gurung, Prajwal Lee, Eung Seok Sharma, Ram Sharma, Mukut |
| description | [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. |
| doi_str_mv | 10.1016/j.bioorg.2021.104681 |
| format | article |
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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.</description><identifier>ISSN: 0045-2068</identifier><identifier>EISSN: 1090-2120</identifier><identifier>DOI: 10.1016/j.bioorg.2021.104681</identifier><identifier>PMID: 33571811</identifier><language>eng</language><publisher>United States: Elsevier Inc</publisher><subject>Alzheimer Disease - diagnosis ; Alzheimer Disease - drug therapy ; Alzheimer Disease - metabolism ; Alzheimer’s disease ; Amyloid beta inhibition ; Animals ; Blood-Brain Barrier - drug effects ; Blood-Brain Barrier - metabolism ; Chalcone ; Chalcone - analogs & derivatives ; Chalcone - chemistry ; Chalcone - therapeutic use ; Cholinesterase inhibitors ; Humans ; Molecular probes ; Molecular Structure ; Multi-target directed ligands ; Neuroinflammation ; Theranostic</subject><ispartof>Bioorganic chemistry, 2021-03, Vol.108, p.104681-104681, Article 104681</ispartof><rights>2021</rights><rights>Published by Elsevier Inc.</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c529t-5218eaec654377dc04436ec5b756ea7ef3112ebcf901c069b37221dbc540492c3</citedby><cites>FETCH-LOGICAL-c529t-5218eaec654377dc04436ec5b756ea7ef3112ebcf901c069b37221dbc540492c3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>230,315,786,790,891,27957,27958</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/33571811$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Thapa, Pritam</creatorcontrib><creatorcontrib>Upadhyay, Sunil P.</creatorcontrib><creatorcontrib>Suo, William Z.</creatorcontrib><creatorcontrib>Singh, Vikas</creatorcontrib><creatorcontrib>Gurung, Prajwal</creatorcontrib><creatorcontrib>Lee, Eung Seok</creatorcontrib><creatorcontrib>Sharma, Ram</creatorcontrib><creatorcontrib>Sharma, Mukut</creatorcontrib><title>Chalcone and its analogs: Therapeutic and diagnostic applications in Alzheimer’s disease</title><title>Bioorganic chemistry</title><addtitle>Bioorg Chem</addtitle><description>[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.</description><subject>Alzheimer Disease - diagnosis</subject><subject>Alzheimer Disease - drug therapy</subject><subject>Alzheimer Disease - metabolism</subject><subject>Alzheimer’s disease</subject><subject>Amyloid beta inhibition</subject><subject>Animals</subject><subject>Blood-Brain Barrier - drug effects</subject><subject>Blood-Brain Barrier - metabolism</subject><subject>Chalcone</subject><subject>Chalcone - analogs & derivatives</subject><subject>Chalcone - chemistry</subject><subject>Chalcone - therapeutic use</subject><subject>Cholinesterase inhibitors</subject><subject>Humans</subject><subject>Molecular probes</subject><subject>Molecular Structure</subject><subject>Multi-target directed ligands</subject><subject>Neuroinflammation</subject><subject>Theranostic</subject><issn>0045-2068</issn><issn>1090-2120</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><recordid>eNp9kc9u1DAQxi0EokvhDRDKkUsWz8R2Eg5I1YoCUiUu5cLFciazu15l7WBnK5UTr8Hr9UlIu6XAhdPInm---fMT4iXIJUgwb3bLzseYNkuUCPOXMg08EguQrSwRUD4WCymVLlGa5kQ8y3knJYCqzVNxUlW6hgZgIb6utm6gGLhwoS_8lOfohrjJb4vLLSc38mHydJfsvduEmO-e4zh4cpOPIRc-FGfD9y37PaebHz_zLMzsMj8XT9ZuyPziPp6KL-fvL1cfy4vPHz6tzi5K0thOpUZo2DEZraq67kkqVRkm3dXasKt5XQEgd7RuJZA0bVfViNB3pJVULVJ1Kt4dfcdDt-eeOEzJDXZMfu_StY3O238zwW_tJl7ZusUGsZoNXt8bpPjtwHmye5-Jh8EFjodsUTUtGtSqmaXqKKUUc068fmgD0t5isTt7xGJvsdgjlrns1d8jPhT95vBnB54PdeU52UyeA3HvE9Nk--j_3-EXxWminw</recordid><startdate>20210301</startdate><enddate>20210301</enddate><creator>Thapa, Pritam</creator><creator>Upadhyay, Sunil P.</creator><creator>Suo, William Z.</creator><creator>Singh, Vikas</creator><creator>Gurung, Prajwal</creator><creator>Lee, Eung Seok</creator><creator>Sharma, Ram</creator><creator>Sharma, Mukut</creator><general>Elsevier Inc</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><scope>5PM</scope></search><sort><creationdate>20210301</creationdate><title>Chalcone and its analogs: Therapeutic and diagnostic applications in Alzheimer’s disease</title><author>Thapa, Pritam ; Upadhyay, Sunil P. ; Suo, William Z. ; Singh, Vikas ; Gurung, Prajwal ; Lee, Eung Seok ; Sharma, Ram ; Sharma, Mukut</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c529t-5218eaec654377dc04436ec5b756ea7ef3112ebcf901c069b37221dbc540492c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2021</creationdate><topic>Alzheimer Disease - diagnosis</topic><topic>Alzheimer Disease - drug therapy</topic><topic>Alzheimer Disease - metabolism</topic><topic>Alzheimer’s disease</topic><topic>Amyloid beta inhibition</topic><topic>Animals</topic><topic>Blood-Brain Barrier - drug effects</topic><topic>Blood-Brain Barrier - metabolism</topic><topic>Chalcone</topic><topic>Chalcone - analogs & derivatives</topic><topic>Chalcone - chemistry</topic><topic>Chalcone - therapeutic use</topic><topic>Cholinesterase inhibitors</topic><topic>Humans</topic><topic>Molecular probes</topic><topic>Molecular Structure</topic><topic>Multi-target directed ligands</topic><topic>Neuroinflammation</topic><topic>Theranostic</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Thapa, Pritam</creatorcontrib><creatorcontrib>Upadhyay, Sunil P.</creatorcontrib><creatorcontrib>Suo, William Z.</creatorcontrib><creatorcontrib>Singh, Vikas</creatorcontrib><creatorcontrib>Gurung, Prajwal</creatorcontrib><creatorcontrib>Lee, Eung Seok</creatorcontrib><creatorcontrib>Sharma, Ram</creatorcontrib><creatorcontrib>Sharma, Mukut</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Bioorganic chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Thapa, Pritam</au><au>Upadhyay, Sunil P.</au><au>Suo, William Z.</au><au>Singh, Vikas</au><au>Gurung, Prajwal</au><au>Lee, Eung Seok</au><au>Sharma, Ram</au><au>Sharma, Mukut</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Chalcone and its analogs: Therapeutic and diagnostic applications in Alzheimer’s disease</atitle><jtitle>Bioorganic chemistry</jtitle><addtitle>Bioorg Chem</addtitle><date>2021-03-01</date><risdate>2021</risdate><volume>108</volume><spage>104681</spage><epage>104681</epage><pages>104681-104681</pages><artnum>104681</artnum><issn>0045-2068</issn><eissn>1090-2120</eissn><notes>ObjectType-Article-1</notes><notes>SourceType-Scholarly Journals-1</notes><notes>ObjectType-Feature-3</notes><notes>content type line 23</notes><notes>ObjectType-Review-2</notes><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.</abstract><cop>United States</cop><pub>Elsevier Inc</pub><pmid>33571811</pmid><doi>10.1016/j.bioorg.2021.104681</doi><tpages>1</tpages><oa>free_for_read</oa></addata></record> |
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| source | ScienceDirect Freedom Collection |
| subjects | Alzheimer Disease - diagnosis Alzheimer Disease - drug therapy Alzheimer Disease - metabolism Alzheimer’s disease Amyloid beta inhibition Animals Blood-Brain Barrier - drug effects Blood-Brain Barrier - metabolism Chalcone Chalcone - analogs & derivatives Chalcone - chemistry Chalcone - therapeutic use Cholinesterase inhibitors Humans Molecular probes Molecular Structure Multi-target directed ligands Neuroinflammation Theranostic |
| title | Chalcone and its analogs: Therapeutic and diagnostic applications in Alzheimer’s disease |
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