2-Aminothiazole: A privileged scaffold for the discovery of anti-cancer agents

Eur J Med Chem. 2021 Jan 15:210:112953. doi: 10.1016/j.ejmech.2020.112953. Epub 2020 Oct 29.

Abstract

Cancer has been the second heath killer being next only to cardiovascular diseases in human society. Although many efforts have been taken for cancer therapy and many achievements have been yielded in the diagnosis and treatment of cancer, the current first-line anti-cancer agents are insufficient owing to the emergence of multi-drug resistance and side effects. Therefore, it is urgent to develop new anti-cancer agents with high activity and low toxicity. 2-Aminothiazole is a class of important scaffold which widely distributes in many natural and synthetic compounds with many pharmacological effects including the potential anti-cancer activity. In this review, we summarized the recent progress of 2-aminothiazole as a privileged scaffold for the discovery of anti-cancer agents based on biological targets, such as tubulin protein, histone acetylase/histone deacetylase (HAT/HDAC), phosphatidylinositol 3-kinases (PI3Ks), Src/Abl kinase, BRAF kinase, epidermal growth factor receptor (EGFR) kinase and sphingosine kinase (SphK), and also investigated the structure-activity relationships (SARs) of most compounds. It is believed that this review could be helpful for medicinal chemists in the discovery of more anti-cancer agents bearing 2-aminothiazole scaffold with excellent activity and high therapeutic index.

Keywords: 2-Aminothiazole; Anti-Cancer; Drug design; Structure-activity relationships.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Drug Design
  • Drug Discovery
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use
  • Structure-Activity Relationship
  • Thiazoles / chemistry*
  • Thiazoles / pharmacology*
  • Thiazoles / therapeutic use
  • Tubulin Modulators / chemistry
  • Tubulin Modulators / pharmacology
  • Tubulin Modulators / therapeutic use

Substances

  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • Thiazoles
  • Tubulin Modulators
  • 2-aminothiazole