Flavones: an important scaffold for medicinal chemistry

Eur J Med Chem. 2014 Sep 12:84:206-39. doi: 10.1016/j.ejmech.2014.07.013. Epub 2014 Jul 5.

Abstract

Flavones have antioxidant, anti-proliferative, anti-tumor, anti-microbial, estrogenic, acetyl cholinesterase, anti-inflammatory activities and are also used in cancer, cardiovascular disease, neurodegenerative disorders, etc. Also, flavonoids are found to have an effect on several mammalian enzymes like protein kinases that regulate multiple cell signaling pathways and alterations in multiple cellular signaling pathways are frequently found in many diseases. Flavones have been an indispensable anchor for the development of new therapeutic agents. The majority of metabolic diseases are speculated to originate from oxidative stress, and it is therefore significant that recent studies have shown the positive effect of flavones on diseases related to oxidative stress. Due to the wide range of biological activities of flavones, their structure-activity relationships have generated interest among medicinal chemists. The outstanding development of flavones derivatives in diverse diseases in very short span of time proves its magnitude for medicinal chemistry research. The present review gives detail about the structural requirement of flavone derivatives for various pharmacological activities. This information may provide an opportunity to scientists of medicinal chemistry discipline to design selective, optimize as well as poly-functional flavone derivatives for the treatment of multi-factorial diseases.

Keywords: Antioxidant; Flavones; Flavonoids; Multi-factorial diseases; Poly-functional.

Publication types

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

MeSH terms

  • Animals
  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / metabolism
  • Anti-Infective Agents / pharmacology
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / metabolism
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Antioxidants / chemistry
  • Antioxidants / metabolism
  • Antioxidants / pharmacology
  • Cardiovascular Diseases / drug therapy
  • Chemistry, Pharmaceutical
  • Flavones / chemistry
  • Flavones / metabolism
  • Flavones / pharmacology*
  • Humans
  • Neoplasms / drug therapy
  • Neoplasms / pathology
  • Neurodegenerative Diseases / drug therapy
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / metabolism
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinases / metabolism
  • Structure-Activity Relationship

Substances

  • Anti-Infective Agents
  • Anti-Inflammatory Agents, Non-Steroidal
  • Antioxidants
  • Flavones
  • Protein Kinase Inhibitors
  • Protein Kinases