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Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors from the natural origin: a recent perspective

Harun M Patel, Rajesh Rane, Neeta Thapliyal

  • 1Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban, 4000, South Africa. karpoormath@ukzn.ac.za.

Anti-Cancer Agents in Medicinal Chemistry
|March 13, 2015
PubMed

Insights

Natural products offer promising avenues for developing novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. This review explores their design, synthesis, and structure-activity relationships for improved cancer treatments.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Natural Products Chemistry

Background:

  • Epidermal growth factor receptor (EGFR) overexpression is prevalent in various human cancers, including prostate, colon, breast, and ovarian.
  • EGFR expression correlates with tumor vascularity and diagnostic challenges.
  • Existing EGFR-tyrosine kinase inhibitors face issues of resistance and significant side effects, necessitating new therapeutic strategies.

Purpose of the Study:

  • To review the design, synthesis, and structure-activity relationships (SAR) of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors derived from natural products.
  • To highlight the potential of natural product-based compounds as alternative or complementary cancer therapies.

Main Methods:

  • Literature review focusing on natural product-derived EGFR inhibitors.
  • Analysis of reported synthetic strategies and SAR studies.
  • Compilation of data on structural modifications and their impact on inhibitory activity.

Main Results:

  • Natural products serve as a rich source for identifying novel scaffolds for EGFR tyrosine kinase inhibitors.
  • Various natural product analogs have demonstrated potent EGFR inhibitory activity.
  • SAR studies reveal key structural features crucial for effective EGFR inhibition.

Conclusions:

  • Natural product-derived compounds represent a promising area for the development of next-generation EGFR inhibitors.
  • Further research into these compounds could lead to more effective and safer anticancer drugs.
  • Exploiting natural product scaffolds can overcome resistance mechanisms associated with current therapies.

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