Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry

Eur J Med Chem. 2019 May 15:170:55-72. doi: 10.1016/j.ejmech.2019.03.004. Epub 2019 Mar 7.

Abstract

The 4-aminoquinazoline core is an interesting pharmacophore and its applications in medicinal chemistry are wide spread. The core has been used for making many kinase inhibitors in past few years. Many researcher demonstrated 4-aminoquinazoline derivatives as specific kinase inhibitors, including tyrosine kinase and serine/theronine kinases. A number of anticancer drugs with 4-aminoquinazoline core are in the market, e.g. gefitinib, erlotinib, afatinib, lapatinib, decomitinib etc. 4-aminoquinazoline derivatives are applied for target specific treatment of lung, breast, colon, prostate cancers. In this review, we discussed the current development of 4-aminoquinazoline derivatives as kinase inhibitors and their uses as anticancer agents in recent years.

Keywords: Aminoquinazoline; Aurora; EGFR; HER; Inhibitor; Kinase; PI3K; Quinazoline; RET; VEGFR.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Chemistry Techniques, Synthetic / methods
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology
  • Protein Kinase Inhibitors / chemical synthesis
  • Protein Kinase Inhibitors / chemistry*
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use*
  • Quinazolines / chemical synthesis
  • Quinazolines / chemistry*
  • Quinazolines / pharmacology
  • Quinazolines / therapeutic use*

Substances

  • 4-aminoquinazoline
  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • Quinazolines