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, M. Hassan, Stefan Bräse, Ahmed Al‐Emam
Abstract
, L858R, T790M, C797S). Computational studies are integrated to reveal binding modes within the ATP-cleft and allosteric pockets, supporting the rational design of next-generation inhibitors. Finally, we identify current challenges-such as off-target toxicity and limited aqueous solubility-and propose future directions for optimizing triazole hybrids toward clinical translation. This scaffold-centric perspective aims to guide medicinal chemists in designing innovative triazole-based EGFR inhibitors with improved efficacy and safety profiles.