An appraisal of anticancer activity with structure-activity relationship of quinazoline and quinazolinone analogues through EGFR and VEGFR inhibition: A review

Drug Dev Res. 2022 Jun;83(4):859-890. doi: 10.1002/ddr.21925. Epub 2022 Mar 16.

Abstract

Cancer is one of the leading causes of death. Globally a huge number of deaths and new incidences are reported annually. Heterocyclic compounds have been proved to be very effective in the treatment of different types of cancer. Among different heterocyclic scaffolds, quinazoline and quinazolinone core were found versatile and interesting with many biological activities. In the discovery of novel anticancer agents, the Quinazoline core is very effective. The FDA has approved more than 20 drugs as an anticancer bearing quinazoline or quinazolinone core in the last two decades. One prime example is Dacomitinib, which was newly approved for non-small-cell lung carcinoma treatment in 2018. These drugs work by different pathways to prevent the spread of cancer cell progression, including inhibition of different kinases, tubulin, kinesin spindle protein, and so forth. This review presented recent developments of quinazoline/quinazolinone scaffold bearing derivatives as anticancer agents acting as epidermal growth factor receptor (EGFR) vascular endothelial growth factor receptor (VEGFR), and dual EGFR/VEGFR inhibitors.

Keywords: EGFR; VEGFR; anticancer; inhibitors; quinazoline; quinazolinone.

Publication types

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

MeSH terms

  • Antineoplastic Agents* / pharmacology
  • Antineoplastic Agents* / therapeutic use
  • Carcinoma, Non-Small-Cell Lung* / drug therapy
  • ErbB Receptors* / antagonists & inhibitors
  • Humans
  • Lung Neoplasms* / drug therapy
  • Quinazolines / pharmacology
  • Quinazolines / therapeutic use
  • Quinazolinones / pharmacology
  • Quinazolinones / therapeutic use
  • Receptors, Vascular Endothelial Growth Factor* / antagonists & inhibitors
  • Structure-Activity Relationship
  • Vascular Endothelial Growth Factor A

Substances

  • Antineoplastic Agents
  • Quinazolines
  • Quinazolinones
  • Vascular Endothelial Growth Factor A
  • EGFR protein, human
  • ErbB Receptors
  • Receptors, Vascular Endothelial Growth Factor