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Chalcone and its analogs: Therapeutic and diagnostic applications in Alzheimer's disease.
Thapa, Pritam; Upadhyay, Sunil P; Suo, William Z; Singh, Vikas; Gurung, Prajwal; Lee, Eung Seok; Sharma, Ram; Sharma, Mukut.
Afiliação
  • Thapa P; Drug Discovery Program, Midwest Veterans' Biomedical Research Foundation, KCVA Medical Center, Kansas City, MO 64128, USA. Electronic address: Pritam.thapa@va.gov.
  • Upadhyay SP; Drug Discovery Program, Midwest Veterans' Biomedical Research Foundation, KCVA Medical Center, Kansas City, MO 64128, USA.
  • Suo WZ; Laboratory for Alzheimer's Disease & Aging Research, Veterans Affairs Medical Center, Kansas City, MO 64128, USA.
  • Singh V; Division of Neurology, KCVA Medical Center, Kansas City, MO, USA.
  • Gurung P; Inflammation Program, University of Iowa, Iowa City, IA 52242, USA.
  • Lee ES; College of Pharmacy, Yeungnam University, Gyeongsan 712-749, Republic of Korea.
  • Sharma R; Drug Discovery Program, Midwest Veterans' Biomedical Research Foundation, KCVA Medical Center, Kansas City, MO 64128, USA.
  • Sharma M; Drug Discovery Program, Midwest Veterans' Biomedical Research Foundation, KCVA Medical Center, Kansas City, MO 64128, USA.
Bioorg Chem ; 108: 104681, 2021 03.
Article em En | MEDLINE | ID: mdl-33571811
Chalcone [(E)-1,3-diphenyl-2-propene-1-one], a small molecule with α, ß 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.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Chalcona / Doença de Alzheimer Tipo de estudo: Diagnostic_studies Limite: Animals / Humans Idioma: En Revista: Bioorg Chem Ano de publicação: 2021 Tipo de documento: Article País de publicação: Estados Unidos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Chalcona / Doença de Alzheimer Tipo de estudo: Diagnostic_studies Limite: Animals / Humans Idioma: En Revista: Bioorg Chem Ano de publicação: 2021 Tipo de documento: Article País de publicação: Estados Unidos