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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.
Abstract:
The Epidermal Growth Factor Receptor (EGFR) and Vascular Endothelial Growth Factor Receptor (VEGFR) families are among the key oncogenic receptors targeted for developing safe and effective drug therapies for cancer. Upon activation, these receptors primarily trigger angiogenesis, a process that plays a crucial role in the proliferation and migration of oncogenic cells by supporting vascularization throughout the body and contributing to tumor growth and metastasis. Some current therapeutic approaches, developed after administration of various models, explored novel drug regimens and established a course of treatment by targeting these receptors. Despite significant progress in this area, the search for more effective and selective anti-cancer agents continues, catering to the need for improved and more advanced therapies. This present review highlights the recent advancements in the development of certain heterocyclic scaffolds targeting these key receptors. The various heterocyclic moieties featured in this review, including derivatives of pyridine, pyrimidine, quinazoline, triazole, and several others, can act as potential antagonists for these receptors and therefore exhibit promising anti-cancer activity. These compounds are supported by their extensive in-vitro studies that not only assess their inhibitory potential but also focus on their structureactivity relationships, pharmacokinetic properties, and toxicity profiles. This review article provides information on the specific compounds found to have the most potent activity against various cancer cell lines evaluated. Therefore, further research on these novel compounds offers substantial prospects for developing potential therapeutic candidates, thereby enhancing cancer treatment.
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.
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