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Article Dans Une Revue Archiv der Pharmazie / Chemistry in Life Sciences Année : 2023

Novel hydrazone‐isatin derivatives as potential EGFR inhibitors: Synthesis and in vitro pharmacological profiling

Marwa Ahmed
Radwan El-Haggar
Atiah Almalki

Résumé

Abstract Merging isatin and arylhydrazone moieties constitutes an efficient strategy to access new potential anticancer derivatives. Consequently, 14 hydrazone‐isatin derivatives were synthesized and evaluated for their antiproliferative activity against the NCI‐60 cancer cell line panel. A kinase assay demonstrated that compound VIIIb inhibited the epidermal growth factor receptor (EGFR), which was confirmed by docking studies, molecular dynamics, and binding free energy calculations. Further characterizations showed that this compound possesses drug‐likeness properties, showed a significant decrease of the cell population in the G2/M phase and led to a significant increase in early and late apoptosis, comparable to erlotinib. Also, VIIIb increased the expression of caspase‐3 and Bax and decreased the expression of Bcl‐2, confirming its potential as a new proapoptotic compound.

Dates et versions

hal-04552606 , version 1 (19-04-2024)

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Marwa Ahmed, Radwan El-Haggar, Atiah Almalki, Omeima Abdullah, Mahmoud El Hassab, et al.. Novel hydrazone‐isatin derivatives as potential EGFR inhibitors: Synthesis and in vitro pharmacological profiling. Archiv der Pharmazie / Chemistry in Life Sciences, 2023, 356 (9), ⟨10.1002/ardp.202300244⟩. ⟨hal-04552606⟩
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