Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton

Eur J Med Chem. 2022 Jan 5:227:113964. doi: 10.1016/j.ejmech.2021.113964. Epub 2021 Nov 1.

Abstract

The tetralone and tetralone derivatives, as crucial structural scaffolds of potential novel drugs targeted at multiple biological end-points, are normally found in several natural compounds and also, it can be used as parental scaffold and/or intermediate for the synthesis of a series of pharmacologically active compounds with a broad-spectrum of bioactivities including antibacterial, antitumor, CNS effect and so on. Meanwhile, SAR information of its analogues has drawn attentions among medicinal chemists, which could contribute to the further research related to tetralone derivatives aimed at multiple targets. This review encompasses pharmacological activities, SAR analysis and docking study of tetralone and its derivatives, expecting to provide a general retrospect and prospect on tetralone derivatives.

Keywords: CNS effect; SAR; Tetralone; antibacterial; antitumor; tetralone derivatives.

Publication types

  • Review

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Bacteria / drug effects*
  • Fluorescent Dyes / chemistry
  • Fluorescent Dyes / pharmacology*
  • Humans
  • Molecular Structure
  • Neoplasms / drug therapy*
  • Tetralones / chemistry
  • Tetralones / pharmacology*

Substances

  • Anti-Bacterial Agents
  • Antineoplastic Agents
  • Fluorescent Dyes
  • Tetralones