Comprehensive Investigation of a Novel Schiff Base: Synthesis, Anticancer Efficacy, Gene Expression Profiling, and Computational Analyses
Tugba Agbektas, Özhan Pazarcı, Ayca Tas, Alakbar Huseynzada, Ruslan Guliyev, Ulviyya Hasanova, Emre Can Buluz, Savas Kaya, Alejandro Morales-Bayuelo, Yavuz Silig
TL;DR
A new compound, B-134-0, shows strong anticancer effects on osteosarcoma cells by affecting DNA repair and cell cycle genes.
Contribution
The study introduces and evaluates B-134-0, a novel azomethine compound with promising anticancer properties.
Findings
B-134-0 showed increasing cytotoxicity over time with IC50 values decreasing from 71.58 to 12.59 μg/mL.
The compound modulated key DNA repair and cell cycle genes like TP53, RAD51, and CDKN1A.
Molecular docking confirmed strong binding affinity with BRCA2 and CDKN1A, aligning with gene expression results.
Abstract
(1) Background: This study evaluates the anticancer potential of a newly synthesized azomethine-based compound, 6,6′,5,8-Dioxa-2,11-diazadodeca-1,11-diene-1,12-diyl)bis(4-bromo-2-methoxyphenol) (B-134-0), against osteosarcoma (SAOS-2) cells, focusing on its effects on apoptosis and DNA-damage-related gene expression. (2) Methods: B-134-0 was synthesized via condensation and tested at eight concentrations (0.5–100 μg/mL) for 24, 48, and 72 h. Cytotoxicity was assessed through MTT assay, and gene expression levels of TP53, RAD51, BRCA2, CASP2, MYC, MDM2, CDKN1A, ERCC1, ATR, and PRKDC were quantified through qPCR using the ΔΔCt method. Molecular docking and DFT analyses were performed to explore structural stability and protein interactions. (3) Results: B-134-0 exhibited strong time-dependent cytotoxicity (IC50: 71.58, 54.36, and 12.59 μg/mL at 24, 48, and 72 h, respectively) and…
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Taxonomy
TopicsCancer-related Molecular Pathways · Synthesis and biological activity · Metal complexes synthesis and properties