Recent Advancements in the Development of Heterocyclic Scaffolds asPotential Anti-cancer Agents Targeting EGFR and VEGFR-2

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.

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Publication Details

Journal
Mini-Reviews in Medicinal Chemistry
Published
2026-06-30
DOI
https://doi.org/10.2174/0113895575448398260627111537
Primary Topic
Synthesis and biological activity
Type
article
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article

Recent Advancements in the Development of Heterocyclic Scaffolds asPotential Anti-cancer Agents Targeting EGFR and VEGFR-2

Twinkle Sharma, Saurabh Sharma, N Jahan, Vindhya Aggarwal et al.
Mini-Reviews in Medicinal Chemistry
Synthesis and biological activity
article

Recent Advancements in the Development of Heterocyclic Scaffolds asPotential Anti-cancer Agents Targeting EGFR and VEGFR-2

Twinkle Sharma, Saurabh Sharma, N Jahan, Vindhya Aggarwal, Apurva Mishra, Sahil Kumar
article en

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.

Mini-Reviews in Medicinal ChemistryVol. 26
Delhi Pharmaceutical Science and Research University (IN)
Openalex Percentile: Top 13%
Synthesis and biological activity
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