Title:Newly Synthesized Arylazo Derivatives Induce Apoptosis and G2/M Cell Cycle Arrest
With Molecular Docking Validation in Human Cancer Cell Lines
Volume: 23
Issue: 10
Author(s): Yara N. Laboud, Nourhan Hassan, Hamdi M. Hassaneen*, Huwaida M. E. Hassaneen, Fatma M. Saleh and Mohamed A. Mohamed Teleb
Affiliation:
- Department of Chemistry, Faculty of Science, Cairo University, Giza, 12613, Egypt
Keywords:
Arylazo derivatives, coupling reaction, cytotoxicity, caspase 3, cell cycle, apoptosis.
Abstract:
Objective: We reported herein the synthesis of novel arylazo derivatives 3a-e incorporating isoquinoline
moiety.
Methods: A coupling reaction of 2-(6,7-dimethoxy-3,4-dihydroisoquinolin-1-yl)acetonitrile 1 with diazotized heterocyclic
amines 2 in ethanol in the presence of sodium acetate to give arylazo derivatives 3a-e.
Results: Cytotoxic effect of five arylazo derivatives on breast carcinoma MCF7 and hepatocellular carcinoma HepG2
was carried out, followed by molecular and functional-based assays, to estimate the anticancer effect of these compounds.
The fibroblast growth factor receptor (FGFR) and epithelial growth factor receptor (EGFR) were found to
interact and bind with the compounds 3a and 3d through several hydrophobic and hydrogen bonds, which were validated
by molecular docking.
Conclusion: The two promising compounds 3a and 3d demonstrated various anticancer potential activities on tumorigenesis,
cytotoxicity, and apoptotic effects, exhibited in the deregulation of the expression of different genes involved
in apoptotic and anti-apoptotic mechanisms, cell cycle arrest at G2/M, and induction of apoptosis in both cell lines.
