Chalcone derivatives: promising starting points for drug design

Marcelo N. Gomes, Eugene N. Muratov, Maristela Pereira, Josana C. Peixoto, Lucimar P. Rosseto, Pedro V.L. Cravo, Carolina H. Andrade, Bruno J. Neves

Research output: Contribution to journalReview articlepeer-review

127 Citations (Scopus)
48 Downloads (Pure)

Abstract

Medicinal chemists continue to be fascinated by chalcone derivatives because of their simple chemistry, ease of hydrogen atom manipulation, straightforward synthesis, and a variety of promising biological activities. However, chalcones have still not garnered deserved attention, especially considering their high potential as chemical sources for designing and developing new effective drugs. In this review, we summarize current methodological developments towards the design and synthesis of new chalcone derivatives and state-of-the-art medicinal chemistry strategies (bioisosterism, molecular hybridization, and pro-drug design). We also highlight the applicability of computer-assisted drug design approaches to chalcones and address how this may contribute to optimizing research outputs and lead to more successful and cost-effective drug discovery endeavors. Lastly, we present successful examples of the use of chalcones and suggest possible solutions to existing limitations.

Original languageEnglish
Article number1210
Pages (from-to)1210-1235
Number of pages25
JournalMolecules
Volume22
Issue number8
DOIs
Publication statusPublished - 1 Aug 2017

Keywords

  • Chalcone derivatives
  • Chalcone synthesis
  • Computer-assisted drug design
  • Molecular modification strategies
  • Natural products

UN Sustainable Development Goals (SDGs)

  • SDG 3 - Good Health and Well-Being

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