Recent Advancements in the Development of Heterocyclic Scaffolds as Potential Anti-cancer Agents Targeting EGFR and

Vindhya Aggarwal1, Saurabh Sharma1, Apurva Mishra1

  • 1Department of Pharmaceutical Chemistry, Delhi Institute of Pharmaceutical Sciences and Research (DIPSAR), Delhi Pharmaceutical Sciences and Research University, New Delhi- 110017, India.

Insights

New heterocyclic compounds show promise as anti-cancer agents by targeting Epidermal Growth Factor Receptor (EGFR) and Vascular Endothelial Growth Factor Receptor (VEGFR). These novel molecules offer potential for developing more effective cancer therapies.

Area of Science:

  • Medicinal Chemistry
  • Oncology
  • Pharmacology

Background:

  • Epidermal Growth Factor Receptor (EGFR) and Vascular Endothelial Growth Factor Receptor (VEGFR) are key oncogenic targets in cancer therapy.
  • Angiogenesis, triggered by these receptors, is crucial for tumor growth, proliferation, and metastasis.
  • Current therapies targeting these receptors have limitations, driving the need for more effective agents.

Purpose of the Study:

  • To review recent advancements in developing heterocyclic scaffolds as antagonists for EGFR and VEGFR.
  • To highlight compounds with promising anti-cancer activity based on in-vitro studies.
  • To explore structure-activity relationships, pharmacokinetics, and toxicity profiles of these novel agents.

Main Methods:

  • Literature review of recent advancements in heterocyclic compounds targeting EGFR and VEGFR.
  • Analysis of in-vitro studies evaluating anti-cancer activity, inhibitory potential, and structure-activity relationships.
  • Assessment of pharmacokinetic properties and toxicity profiles of promising compounds.

Main Results:

  • Several heterocyclic scaffolds, including pyridine, pyrimidine, quinazoline, and triazole derivatives, show potential as EGFR and VEGFR antagonists.
  • These compounds exhibit promising anti-cancer activity against various cancer cell lines.
  • In-vitro studies provide data on inhibitory potential, SAR, pharmacokinetics, and toxicity.

Conclusions:

  • Novel heterocyclic compounds represent a promising avenue for developing targeted anti-cancer therapies.
  • Further research into these compounds could lead to the development of potent therapeutic candidates.
  • These agents have the potential to enhance existing cancer treatment strategies.