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Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Thiazole-driven heterocyclic hybrids as EGFR inhibitors: progress in synthesis and anticancer applications
Ancilla Dsouza1, V M Subrahmanyam2, Nitinkumar S Shetty1
1Department of Chemistry, Manipal Institute of Technology, Manipal Academy of Higher Education Manipal Karnataka 576104 India nitin.shetty@manipal.edu.
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.
Insights
This review explores novel thiazole hybrid compounds as epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) for cancer therapy. Despite challenges like resistance, these TKIs show promise for improved cancer treatment strategies.
Area of Science:
- Oncology
- Medicinal Chemistry
- Molecular Biology
Background:
- Cancer remains a major global health challenge, necessitating advanced therapeutic strategies.
- Targeting the epidermal growth factor receptor (EGFR) signaling pathway is a crucial approach in cancer treatment.
- Inhibiting the EGFR tyrosine kinase domain has shown significant therapeutic benefits.
Purpose of the Study:
- To review the current landscape of EGFR inhibitors in cancer treatment.
- To highlight recent advancements in the design and synthesis of novel thiazole hybrid compounds as potential EGFR TKIs.
- To address challenges such as epigenetic mutations and acquired resistance affecting TKI efficacy.
Main Methods:
- Review of existing literature on EGFR inhibitors and cancer therapy.
- Focus on molecular modeling techniques for designing small molecules.
- Emphasis on the synthesis and development of thiazole hybrid compounds.
Main Results:
- Numerous thiazole-based hybrid small molecules have been developed as potential EGFR TKIs.
- Understanding genetic alterations in the EGFR tyrosine kinase domain is key to developing potent inhibitors.
- Challenges like resistance necessitate ongoing research for improved therapeutic efficacy.
Conclusions:
- Thiazole hybrid compounds represent a promising class of selective EGFR TKIs.
- Continued research is vital to overcome resistance mechanisms and enhance long-term efficacy of EGFR inhibitors.
- Novel EGFR TKIs are crucial for advancing cancer treatment strategies.
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