Current progress of 1,2,3-triazole hybrids as EGFR inhibitors for cancer therapy – a literature review

Hussam Elddin Nabeih Khasawneh, Hesham M. Hassan, Amal Ali Alharbi, Wesam Taher Almagharbeh, Raed Fanoukh Aboqader Al-Aouadi, Kirandeep Kaur, Ramya Maranan, Hadeer M. Farhan, Hamada Hashem, Mariam M. Hassan, Stefan Bräse and Ahmed Al-Emam

RSC Adv., 2025,15, 40998-41047

Abstract

Epidermal growth factor receptor (EGFR) is a validated oncogenic driver in numerous solid tumors, and resistance to first- and second-generation tyrosine kinase inhibitors continues to limit clinical outcomes.

Design, synthesis, and characterization of novel 5-ethylsulfonyl-indazole-3-carboxamides as dual VEGFR-2 and EGFR inhibitors: apoptotic antiproliferative and immunomodulatory evaluations

Lamya H. Al-Wahaibi, Shimaa A. Othman, Hesham A. Abou-Zied, Stefan Bräse, Bahaa G. M. Youssif and Safwat M. Rabea

RSC Adv., 2025,15, 47710-47734

Abstract

This study focused on the development of a novel series of 5-ethylsulfonyl-indazole-3-carboxamides (8a–l) as dual inhibitors of VEGFR-2 and EGFR. Compounds 8g and 8h emerged as the most potent derivatives against breast (MCF-7) and colorectal (HCT-116) cancer cell lines.

Design and evaluation of sulfadiazine derivatives as potent dual inhibitors of EGFR^WT and EGFR^T790M: integrating biological, molecular docking, and ADMET analysis

Hany M. Abd El-Lateef, Hend A. A. Ezelarab, Ali M. Ali, Azhaar T. Alsaggaf, Wael A. Mahdi, Sultan Alshehri, Mohamed A. El Hamd and Moustafa O. Aboelez

RSC Adv., 2024,14, 28608-28625

Abstract

A series of derivatives (5–14) were synthesized through the diazotization of sulfadiazine with active methylene compounds.

Design, synthesis, and apoptotic antiproliferative activity of novel dihydropyrimidine-5-carbonitrile/1,2,4-oxadiazole hybrids as dual EGFR/VEGFR-2 inhibitors endowed with antioxidant activity

Lamya H. Al-Wahaibi, Amira M. Mohamed, Hesham A. Abou-Zied, Abdullah Yahya Abdullah Alzahrani, Stefan Bräse and Bahaa G. M. Youssif

RSC Adv., 2025,15, 38998-39027

Abstract

A series of new dihydropyrimidine/1,2,4-oxadiazole compounds was designed and synthesised. Their structures were validated by IR, NMR, and elemental analysis, and they were evaluated as antiproliferative agents targeting EGFR and VEGFR-2.

Design, synthesis, and biological evaluation of new pyrimidine-5-carbonitrile derivatives as novel anti-cancer, dual EGFR^WT/COX-2 inhibitors with docking studies

Nada Reda, Ahmed Elshewy, Hesham I. EL-Askary, Khaled O. Mohamed and Amira A. Helwa

RSC Adv., 2023,13, 32296-32320

Abstract

A series of pyrimidine-5-carbonitriles was designed and synthesized as potential anti-cancer agents with dual EGFR^WT/COX-2 inhibition. Compounds 4e and 4f disclosed the highest activity on all NCI60 cell lines.

Current progress of 1,2,3-triazole hybrids as EGFR inhibitors for cancer therapy – a literature review

Abstract

Design, synthesis, and characterization of novel 5-ethylsulfonyl-indazole-3-carboxamides as dual VEGFR-2 and EGFR inhibitors: apoptotic antiproliferative and immunomodulatory evaluations

Abstract

Design and evaluation of sulfadiazine derivatives as potent dual inhibitors of EGFRWT and EGFRT790M: integrating biological, molecular docking, and ADMET analysis

Abstract

Design, synthesis, and apoptotic antiproliferative activity of novel dihydropyrimidine-5-carbonitrile/1,2,4-oxadiazole hybrids as dual EGFR/VEGFR-2 inhibitors endowed with antioxidant activity

Abstract

Design, synthesis, and biological evaluation of new pyrimidine-5-carbonitrile derivatives as novel anti-cancer, dual EGFRWT/COX-2 inhibitors with docking studies

Abstract

Design and evaluation of sulfadiazine derivatives as potent dual inhibitors of EGFR^WT and EGFR^T790M: integrating biological, molecular docking, and ADMET analysis

Design, synthesis, and biological evaluation of new pyrimidine-5-carbonitrile derivatives as novel anti-cancer, dual EGFR^WT/COX-2 inhibitors with docking studies