# Thiazole–driven heterocyclic hybrids as EGFR inhibitors: progress in synthesis and anticancer applications

**Authors:** Ancilla Dsouza, V. M. Subrahmanyam, Nitinkumar S. Shetty

PMC · DOI: 10.1039/d5ra04838a · RSC Advances · 2026-01-02

## TL;DR

This paper reviews recent advances in developing thiazole-based compounds as inhibitors of the EGFR tyrosine kinase for cancer treatment.

## Contribution

The paper highlights novel thiazole hybrid compounds as promising selective EGFR tyrosine kinase inhibitors.

## Key findings

- Thiazole-based hybrids show potential as selective EGFR tyrosine kinase inhibitors.
- Molecular modeling techniques have been used to design these compounds.
- Challenges like resistance and mutations remain, necessitating further research.

## Abstract

Despite considerable progress in therapeutic developments, cancer still stands as one of the most common and lethal health challenges worldwide. Targeting the EGFR signaling pathway has emerged as a key approach in cancer therapy. Inhibiting the intracellular tyrosine kinase domain of EGFR has demonstrated significant therapeutic benefits. To discover effective EGFR tyrosine kinase inhibitors (TKIs), numerous small molecules, particularly thiazole-based hybrids have been developed using molecular modelling techniques. However, challenges such as epigenetic mutations and acquired resistance have limited their long-term efficacy, highlighting the need for continued research in this area. Recent efforts have focused on understanding genetic alterations within the EGFR tyrosine kinase domain, paving the way for the development of more selective and potent inhibitors. This review presents an overview of the role and current landscape of EGFR inhibitors in cancer treatment, with a particular emphasis on recent progress in the design, synthesis, and development of novel thiazole hybrid compounds as promising selective EGFR TKIs.

An overview of the role and current landscape of EGFR inhibitors in cancer treatment, with a particular emphasis on recent progress in the design, synthesis, and development of novel thiazole hybrid compounds as promising selective EGFR TKIs.

## Linked entities

- **Genes:** EGFR (epidermal growth factor receptor) [NCBI Gene 1956]
- **Chemicals:** thiazole (PubChem CID 9256)
- **Diseases:** cancer (MONDO:0004992)

## Full-text entities

- **Genes:** EGFR (epidermal growth factor receptor) [NCBI Gene 1956] {aka ERBB, ERBB1, ERRP, HER1, NISBD2, NNCIS}, TXK (TXK tyrosine kinase) [NCBI Gene 7294] {aka BTKL, PSCTK5, PTK4, RLK, TKL}
- **Diseases:** cancer (MESH:D009369)
- **Chemicals:** Thiazole (MESH:D013844)

## Full text

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## Figures

76 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12757916/full.md

## References

82 references — full list in the complete paper: https://tomesphere.com/paper/PMC12757916/full.md

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Source: https://tomesphere.com/paper/PMC12757916