Design, synthesis and computational evaluation of 1,2,3-triazole-Schiff base hybrid as AKT1 inhibitor for breast cancer

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Authors: Obaid Afzal, Mohamed Enneiymy, Shamsa Bibi, Hassan A Madkhali, Taibah Aldakhil, Bharath Kumar Chagaleti, Samreen Gul Khan, Yassine Riadi, Ali Altharawi, Reda A. Haggam
Cited by: 3
References: 72

Abstract

Cancer remains a major global health problem, with breast cancer being one of the most common malignancies. The PI3K/AKT/mTOR pathway, in particular the AKT1 kinase, plays a key role in tumour progression and resistance to treatment. This study focuses on the synthesis and evaluation of novel triazole-Schiff base hybrid compounds as potential AKT1 inhibitors. The hybrid molecules were synthesised using a multi-step process, characterised using spectroscopic techniques and subjected to extensive computational analysis, including density functional theory (DFT), molecular docking, molecular dynamics simulations and ADMET profiling. The results showed that the synthesised compound 5 exhibited a high binding affinity to AKT1 (-9.0 kcal/mol), higher than that of the reference drug Capivasertib (-7.46 kcal/mol). Network pharmacology identified key targets such as AKT1, EGFR and mTOR, while toxicity predictions indicated a favourable safety profile. These results highlight the potential of triazole-Schiff base hybrid as promising candidates for breast cancer therapy, warranting further experimental validation.

Fields of Study & Subjects

PI3K/AKT/mTOR signaling in cancer Synthesis and biological activity Click Chemistry and Applications

Publication details

Journal / source
Chemical Physics Impact
Publisher
Elsevier BV
Volume
12
Pages
101001–101001
Publication date
5 January 2026
Language
EN