Anticancer Active Heterocyclic Chalcones: Recent Developments

Anticancer Agents Med Chem. 2021;21(5):558-566. doi: 10.2174/1871520620666200705215722.

Abstract

Background: Chalcones are structurally simple compounds that are easily accessible by synthetic methods. Heterocyclic chalcones have gained the interest of scientists due to their diverse biological activities. The anti-tumor activities of heterocyclic chalcones are especially remarkable and the growing number of publications dealing with this topic warrants an up-to-date compilation.

Methods: Search for antitumor active heterocyclic chalcones was carried out using Pubmed and Scifinder as common web-based literature searching tools. Pertinent and current literature was covered from 2015/2016 to 2019. Chemical structures, biological activities and modes of action of anti-tumor active heterocyclic chalcones are summarized.

Results: Simply prepared chalcones have emerged over the last years with promising antitumor activities. Among them, there are a considerable number of tubulin polymerization inhibitors. But there are also new chalcones targeting special enzymes such as histone deacetylases or with DNA-binding properties.

Conclusion: This review provides a summary of recent heterocyclic chalcone derivatives with distinct antitumor activities.

Keywords: Chalcone; anticancer agents; drug design; heterocycle; histone deacetylase; tubulin.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Chalcones / chemical synthesis
  • Chalcones / chemistry
  • Chalcones / pharmacology*
  • Drug Development*
  • Drug Screening Assays, Antitumor
  • Heterocyclic Compounds / chemical synthesis
  • Heterocyclic Compounds / chemistry
  • Heterocyclic Compounds / pharmacology*
  • Humans
  • Molecular Structure
  • Neoplasms / drug therapy*
  • Neoplasms / pathology

Substances

  • Antineoplastic Agents
  • Chalcones
  • Heterocyclic Compounds