A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs

Bioorg Med Chem. 2019 Mar 1;27(5):677-685. doi: 10.1016/j.bmc.2019.01.027. Epub 2019 Jan 26.

Abstract

Protein kinases have been important targets for antitumor targets due to their key roles in regulating multiple cell signaling pathways. Numerous compounds containing flavonoid scaffold as an indispensable anchor have been found to be potent inhibitors of protein kinases. Some of these flavonoids have been in clinical research as protein kinases inhibitors. Thus, the present review mainly focuses on the structural requirement for anticancer potential of flavone derivatives targeting several key serine/threonine protein kinases. This information may provide an opportunity to scientists of medicinal chemistry to design multi-functional flavone derivatives for the treatment of cancer.

Keywords: Binding mode; Cancer; Flavonoids; Protein kinase; Structure-activity relationship.

Publication types

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

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / metabolism
  • Antineoplastic Agents / therapeutic use*
  • Flavones / chemistry
  • Flavones / metabolism
  • Flavones / therapeutic use*
  • Humans
  • Neoplasms / drug therapy*
  • Protein Binding
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / metabolism
  • Protein Kinase Inhibitors / therapeutic use*
  • Protein Serine-Threonine Kinases / antagonists & inhibitors*
  • Protein Serine-Threonine Kinases / chemistry
  • Protein Serine-Threonine Kinases / metabolism

Substances

  • Antineoplastic Agents
  • Flavones
  • Protein Kinase Inhibitors
  • Protein Serine-Threonine Kinases