Recent development of heterocyclic scaffolds as EGFR kinase inhibitors in cancer

The Epidermal Growth Factor Receptor (EGFR) is responsible for cell differentiation and proliferation upon activation when it binds to one of its ligands. It is thought to be involved tumorigenesis, which is implicated in cancers such as lung cancer and breast cancer. Over the past decades, the EGFR has become extensively examined as a target for the development of new anticancer agents. Several EGFR tyrosine kinase inhibitors (TKIs) have been identified and assessed in clinical trials as potential treatments for carcinoma. This review provides updated information on Novel heterocyclic scaffolds, which are now considered important pharmacophores that have demonstrated significant potency as EGFR inhibitors. Kinase inhibitors, in the last few years, have emerged as emerging anticancer agents with promising results. In this review, we briefly discussed heterocyclic scaffolds and the structural activity relationships of lead compounds such as substituted quinazoline, pyrimidine, quinoline and indole as EGFR kinase inhibitors, as well as their use as anticancer agents. Information on miscellaneous heterocyclics such as thiazolyl-pyrazoline derivatives, pyrazole derivatives and oxadiazole derivatives is also included. Słowa kluczowe: cancer, heterocyclic scaffolds, kinase inhibitors

Authors

Publication Details

Journal
Current Issues in Pharmacy and Medical Sciences
Published
2025-05-21
DOI
https://doi.org/10.12923/cipms-2025-0018
Primary Topic
HER2/EGFR in Cancer Research
Type
article
Field-Weighted Citation Impact
0.00
Controls
|||
ALL TIME
JAN
FEB
MAR
APR
MAY
JUN
JUL
AUG
SEP
OCT
article

Recent development of heterocyclic scaffolds as EGFR kinase inhibitors in cancer

Rupali Likhar, Shrikant V. Joshi
Current Issues in Pharmacy and Medical Sciences
HER2/EGFR in Cancer Research
article

Recent development of heterocyclic scaffolds as EGFR kinase inhibitors in cancer

Rupali Likhar, Shrikant V. Joshi
article en

Abstract

The Epidermal Growth Factor Receptor (EGFR) is responsible for cell differentiation and proliferation upon activation when it binds to one of its ligands. It is thought to be involved tumorigenesis, which is implicated in cancers such as lung cancer and breast cancer. Over the past decades, the EGFR has become extensively examined as a target for the development of new anticancer agents. Several EGFR tyrosine kinase inhibitors (TKIs) have been identified and assessed in clinical trials as potential treatments for carcinoma. This review provides updated information on Novel heterocyclic scaffolds, which are now considered important pharmacophores that have demonstrated significant potency as EGFR inhibitors. Kinase inhibitors, in the last few years, have emerged as emerging anticancer agents with promising results. In this review, we briefly discussed heterocyclic scaffolds and the structural activity relationships of lead compounds such as substituted quinazoline, pyrimidine, quinoline and indole as EGFR kinase inhibitors, as well as their use as anticancer agents. Information on miscellaneous heterocyclics such as thiazolyl-pyrazoline derivatives, pyrazole derivatives and oxadiazole derivatives is also included. Słowa kluczowe: cancer, heterocyclic scaffolds, kinase inhibitors

Current Issues in Pharmacy and Medical SciencesVol. 38(2)
Openalex Percentile: Top 80%
HER2/EGFR in Cancer Research
AI Navigator

Ask Laika to Summarize, Analyze, and Connect papers live on the map.

Summarize Papers & Methodologies

Extract key findings, datasets, and comparative methods across publications.

Benchmark Rankings & Visual Analytics

Rank top research institutions, authors, funders, topics, and journals by Field-Weighted Citation Impact (FWCI) and paper volume with instant charts.

Connect Distant Disciplines

Bridge topological clusters on the map to find hidden collaborative intersections.