Literature DB >> 30773996

Recent developments in biological aspects of chalcones: the odyssey continues.

Anu Rani1, Amit Anand2, Kewal Kumar3, Vipan Kumar1.   

Abstract

INTRODUCTION: Chalcones are attractive to synthetic chemists because they are easy to prepare, have a large number of replaceable hydrogens, thereby having significant biological potential. Chalcones and their derivatives (carbocyclic as well as heterocyclic) exhibit a range of biological properties including anticancer, antimalarial, antioxidant, anti-inflammatory and anti-tubercular activities. Their promising biological profile, along with their ease of synthetic manipulations, have triggered the design and development of new chalcone derivatives as well as their conjugates with active pharmacophores affording therapeutic templates targeting various diseases. Areas covered: This review focuses on synthesized substituted chalcones as well as chalcone-based molecular conjugates that have been developed between 2015 and 2018. Furthermore, their structure-activity relationships with an emphasis on their mechanism of action and docking studies along with their future therapeutic applications. Expert opinion: A recent upsurge in scientific literature encompassing the synthesis of new chalcone-derivatives as well as its role in ameliorating the activity profiles via amalgamation with other pharmacophores has clearly established the importance of chalcones in present-day drug discovery. As a point, we, the authors, believe that new effective scaffolds can be developed from chalcones with an added advantage of being available at a low cost.

Entities:  

Keywords:  Claisen-schmidt condensation; Structutre Activity Relationship (SAR); anti-malarial; anti-oxidant; anti-proliferatives; chalcones

Year:  2019        PMID: 30773996     DOI: 10.1080/17460441.2019.1573812

Source DB:  PubMed          Journal:  Expert Opin Drug Discov        ISSN: 1746-0441            Impact factor:   6.098


  5 in total

1.  Hydroxylated Chalcones as Aryl Hydrocarbon Receptor Agonists: Structure-Activity Effects.

Authors:  Hyejin Park; Un-Ho Jin; Keshav Karki; Clinton Allred; Laurie A Davidson; Robert S Chapkin; Asuka A Orr; Farrhin Nowshad; Arul Jayaraman; Phanourios Tamamis; Stephen Safe
Journal:  Toxicol Sci       Date:  2021-02-26       Impact factor: 4.849

2.  Synthesis, inverse docking-assisted identification and in vitro biological characterization of Flavonol-based analogs of fisetin as c-Kit, CDK2 and mTOR inhibitors against melanoma and non-melanoma skin cancers.

Authors:  Tithi Roy; Samuel T Boateng; Sergette Banang-Mbeumi; Pankaj K Singh; Pratik Basnet; Roxane-Cherille N Chamcheu; Federico Ladu; Isabel Chauvin; Vladimir S Spiegelman; Ronald A Hill; Konstantin G Kousoulas; Bolni Marius Nagalo; Anthony L Walker; Jean Fotie; Siva Murru; Mario Sechi; Jean Christopher Chamcheu
Journal:  Bioorg Chem       Date:  2020-12-30       Impact factor: 5.275

3.  Identification of new fisetin analogs as kinase inhibitors: Data on synthesis and anti-skin cancer activities evaluation.

Authors:  Tithi Roy; Samuel T Boateng; Sergette Banang-Mbeumi; Pankaj K Singh; Pratik Basnet; Roxane-Cherille N Chamcheu; Federico Ladu; Isabel Chauvin; Vladimir S Spiegelman; Ronald A Hill; Konstantin G Kousoulas; Bolni Marius Nagalo; Anthony L Walker; Jean Fotie; Siva Murru; Mario Sechi; Jean Christopher Chamcheu
Journal:  Data Brief       Date:  2021-02-10

Review 4.  Exploration of chalcones and related heterocycle compounds as ligands of adenosine receptors: therapeutics development.

Authors:  Chrisna Matthee; Gisella Terre'Blanche; Lesetja J Legoabe; Helena D Janse van Rensburg
Journal:  Mol Divers       Date:  2021-06-27       Impact factor: 3.364

5.  Synthesis of Biobased Phloretin Analogues: An Access to Antioxidant and Anti-Tyrosinase Compounds for Cosmetic Applications.

Authors:  Laurène Minsat; Cédric Peyrot; Fanny Brunissen; Jean-Hugues Renault; Florent Allais
Journal:  Antioxidants (Basel)       Date:  2021-03-25
  5 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.