Discovery of a Uracil‐Derived Small Organic Ligand with Cytotoxic Effect on Human PC‐3 Cell Lines via Apoptosis
Year: 2024
Type: article
Abstract: A series of novel 6‐amino‐5‐salicylidene uracils (1–19) were efficiently synthesized from the condensation reaction of 5,6‐diamino‐1,3‐dimethyluracil with substituted salicylaldehydes. The structural characterization of the compounds was performed with spectroscopic methods and elemental analysis. All compounds were evaluated for their in vitro cytotoxic activity against PC‐3 (human prostate adenocarcinoma), A549 (human alveolar adenocarcinoma) and SHSY‐5Y (human neuroblastoma) cancer cell lines. 3,5‐di‐ tert ‐Butylsalicylaldehyde derived salicylideneuracil (6ASU‐8) showed promising cytotoxic activity against PC‐3 cells with an IC 50 value of 1.53±1.01 μM, compared to doxorubicin, which had an IC 50 value of 3.77±1.34 μM. 6ASU‐8 induced cell cycle arrest at the G2/M phase and promoted apoptosis in PC‐3 cells ( p <0.05*). Molecular docking results supported the experimental data, indicating that 6ASU‐8 is more effective than doxorubicin. Additionally, in silico ADME analysis revealed that 6ASU‐8 possesses acceptable predictive physicochemical properties.
Source: ChemistrySelect
Authors: Ayşe Halıç Poslu, Rümeysa Balaban, Ayşe Nalbantsoy, Onur Ertik, Gülşah Çeçener, Ömer Koz, Gamze Koz
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: green
OpenAlex ID: W4402732815