Synthesis Optimization and SNEDDS Formulation of 1-(2,5-Dihydroxyphenyl)-(3-pyridin-2- yl)-propenone: Enhanced In Vitro Cytotoxicity on HeLa Cells

Objective This study aims to optimize the synthesis conditions (catalyst concentration and reaction time) to improve yield, enhance compound purity, and establish an equation for yield calculation. Additionally, the synthesized compound was tested in vitro on HeLa cells to assess its pharmacological activity against cervical cancer. Methods The synthesis was conducted using 2,5-dihydroxyacetophenone and pyridine-2-carbaldehyde in a basic medium (Na ₂ CO ₃ ) under microwave irradiation at 70°C for 45 minutes. Variations in Na ₂ CO ₃ concentration (0.0001 to 0.001 mol) and reaction time (30 to 90 minutes) were explored. The purity of the compound was evaluated using TLC and melting point analysis. In vitro cytotoxicity was assessed using the MTT assay. Key Findings : The TLC test revealed a single spot, and the melting point (185.5°C – 186.1°C) confirmed purity. The optimized catalyst concentration (0.0006 mol Na₂CO₃) yielded 43.33% after purification, while the optimal reaction time (75 minutes) resulted in a 74.44% yield. The in vitro assay demonstrated that the SNEDDS formulation significantly enhanced cytotoxic activity, with an IC₅₀ of 2.6 µg/mL, compared to the non-SNEDDS formulation, which exhibited an IC₅₀ of 4.17 µg/mL. This suggests that SNEDDS improved drug solubility and cellular uptake, resulting in enhanced anticancer potency against HeLa cells. Conclusion This study successfully optimized the synthesis of 1-(2,5-dihydroxyphenyl)-(3-pyridin-2-yl)-propenone, improving its yield and purity. Furthermore, the SNEDDS formulation significantly increased cytotoxic efficacy, highlighting the compound’s potential as promising anticancer agent for cervical cancer treatment.