1,2,3-Triazole-Based Hybrids as EGFR Inhibitors: An overview

Yassen, Asmaa SA; Nawareg, Nareman A.; Husseiny, Ebtehal M.; El-Sayed, Magda A. A.; Elshihawy, Hosam A.

doi:10.21608/rpbs.2025.389927.1379

	1,2,3-Triazole-Based Hybrids as EGFR Inhibitors: An overview
Records of Pharmaceutical and Biomedical Sciences
Volume 9, Issue 1, March 2025, Page 84-91 PDF (760.95 K)
Document Type: Mini-reviews
DOI: 10.21608/rpbs.2025.389927.1379
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Authors
Asmaa SA Yassen ¹; Nareman A. Nawareg²; Ebtehal M. Husseiny³; Magda A. A. El-Sayed⁴; Hosam A. Elshihawy¹
¹Pharmaceutical Organic Chemistry, School of Pharmacy, Suez Canal University
²Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Horus University, New Damietta 34518, Egypt.
³Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy (Girls), Al-Azhar University, Nasr City, Cairo 11754, Egypt
⁴Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
Abstract
Cancer continues to be a leading cause of mortality worldwide, presenting a major global public health concern. Despite advances in treatment, the discovery and development of effective anticancer drugs remain significant challenges for medicinal chemists. Among key therapeutic targets, the epidermal growth factor receptor (EGFR) plays a crucial role in cancer progression, with its overexpression and oncogenic mutations closely linked to tumor development and multidrug resistance. Nitrogen-containing heterocycles, especially 1,2,3-triazoles, have garnered substantial interest in drug discovery due to their structural resemblance to natural biomolecules and their broad pharmacological potential. Over the past decade, the 1,2,3-triazole scaffold has demonstrated promising anticancer activity, with compounds such as CAI and Cefatrizine serving as notable examples. Additionally, several 1,2,3-triazole-based hybrids have exhibited potent EGFR inhibitory effects, suggesting a valuable avenue for targeted therapy. This review covers synthetic methods for 1,2,3-triazoles and highlights recent advancements in the development of 1,2,3-triazole-containing EGFR inhibitors reported between 2019 and 2024.
Keywords
Anticancer; EGFR; Synthesis; Inhibition; 1; 2; 3-triazole; Hybrids; Inhibitors


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